Cat. No.: HY-15772

Osimertinib

(Synonyms: AZD-9291; Mereletinib)

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Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

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Pureté: 99.69%
CAS No.: 1421373-65-0
Formule: C₂₈H₃₃N₇O₂
Masse moléculaire:499.61

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Osimertinib Chemical Structure

CAS No.: 1421373-65-0

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Activité biologique
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- IC₅₀ & Target
- Cellular Effect
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Publications (202)
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Description

IC₅₀ & Target^[1]

EGFR^L858R

12 nM (IC₅₀, Enzyme assays)

EGFR^L858R/T790M

1 nM (IC₅₀, Enzyme assays)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.893 μM Compound: AZD9291	Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay	[PMID: 27131639]
A-431	IC₅₀	1.604 μM Compound: 3	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay	[PMID: 28033579]
A-431	IC₅₀	615.6 nM Compound: AZD9291	Antiproliferative activity against human A431 cells harboring wild-type EGFR Antiproliferative activity against human A431 cells harboring wild-type EGFR	[PMID: 28426996]
A-431	EC₅₀	0.7 μM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
A-431	EC₅₀	0.67 μM Compound: Osimertinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A-431	IC₅₀	0.956 μM Compound: 3; AZD9291	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay	[PMID: 28987609]
A-431	IC₅₀	0.685 μM Compound: AZD-9291	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay	[PMID: 29534926]
A-431	IC₅₀	1.26 μM Compound: 5; AZD9291	Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay	[PMID: 29730192]
A-431	IC₅₀	1.24 μM Compound: AZD9291	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay	[PMID: 30429956]
A-431	GI₅₀	40.1 nM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
A-431	IC₅₀	0.61 μM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
A-431	IC₅₀	0.945 μM Compound: 6; AZD-9291	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay	[PMID: 30471829]
A-431	IC₅₀	1.44 μM Compound: 4; AZD9291	Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay	[PMID: 31223440]
A-431	CC₅₀	967 nM Compound: Osimertinib	Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]
A-431	IC₅₀	84 nM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
A-431	IC₅₀	1.19 μM Compound: 4	Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
A-431	IC₅₀	1.3 μM Compound: 4	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
A-431	IC₅₀	0.4 μM Compound: AZD9291	Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay	[PMID: 31889606]
A-431	IC₅₀	0.85 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
A-431	IC₅₀	1.51 μM Compound: 6, AZD9291	Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay	[PMID: 32631532]
A-431	IC₅₀	0.77 μM Compound: AZD9291	Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A-431	IC₅₀	742 nM Compound: AZD9291	Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
A-431	IC₅₀	138.7 nM Compound: AZD9291	Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay	[PMID: 33459024]
A-431	IC₅₀	5.32 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33640672]
A-431	IC₅₀	795.2 nM Compound: AZD9291	Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay	[PMID: 33667898]
A-431	IC₅₀	1.226 μM Compound: AZD9291	Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34218082]
A-431	IC₅₀	0.77 μM Compound: AZD9291	Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay	[PMID: 34534838]
A-431	IC₅₀	1310 nM Compound: Osimertinib	Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
A-431	IC₅₀	2.035 nM Compound: 5	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
A-431	IC₅₀	0.821 μM Compound: AZD9291	Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
A-431	EC₅₀	0.956 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	GI₅₀	0.596 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	IC₅₀	1.325 μM Compound: 4	Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36288657]
A-431	CC₅₀	550 nM Compound: 6; AZD9291	Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay	[PMID: 36749735]
A-431	IC₅₀	0.619 μM Compound: 6	Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]
A-431	EC₅₀	830 nM Compound: 1	Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
A-431	IC₅₀	1.31 μM Compound: 5; AZD9291	Antiproliferative activity against human A-431 cells by MTT assay Antiproliferative activity against human A-431 cells by MTT assay	[PMID: 37336419]
A-431	GI₅₀	619 nM Compound: Osi; AZD9291	Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
A-431	IC₅₀	1.4 μM Compound: 2	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37839342]
A-431	IC₅₀	0.92 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 37885208]
A-431	IC₅₀	2.64 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
A-431	IC₅₀	795.2 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38879996]
A-431	IC₅₀	0.821 μM Compound: AZD9291	Cytotoxicity against human A-431 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human A-431 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
A549	IC₅₀	150 nM Compound: 9; AZD9291	Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA	[PMID: 26756222]
A549	GI₅₀	3.5 μM Compound: 5; AZD9291	Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
A549	EC₅₀	1.83 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A549	IC₅₀	0.53 μM Compound: AZD	Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29466773]
A549	IC₅₀	0.87 μM Compound: AZD9291	Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay	[PMID: 29486953]
A549	IC₅₀	486 nM Compound: AZD9291	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29576272]
A549	IC₅₀	0.53 μM Compound: osimertinib	Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29853340]
A549	IC₅₀	0.31 μM Compound: 2	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay	[PMID: 30108918]
A549	IC₅₀	3.242 μM Compound: 6; AZD-9291	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30471829]
A549	IC₅₀	0.615 μM Compound: 6; AZD9291	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30530173]
A549	IC₅₀	5 μM Compound: Osimertinib	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
A549	IC₅₀	0.462 μM Compound: 3; AZD9291	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31683104]
A549	IC₅₀	0.72 μM Compound: 4	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
A549	IC₅₀	0.14 μM Compound: AZD9291	Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 31889606]
A549	IC₅₀	0.9 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
A549	IC₅₀	0.67 μM Compound: AZD9291	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A549	IC₅₀	1.97 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 32961382]
A549	IC₅₀	0.672 μM Compound: AZD9291	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay	[PMID: 34534838]
A549	IC₅₀	0.335 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay	[PMID: 34794818]
A549	IC₅₀	0.784 μM Compound: AZD9291	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
A549	IC₅₀	0.445 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
A549	IC₅₀	1.87 μM Compound: 3	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]
A549	IC₅₀	0.92 μM Compound: Osimertinib	Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
A549	IC₅₀	2.67 μM Compound: Osimertinib	Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
A549	IC₅₀	0.682 μM Compound: 6	Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]
A549	IC₅₀	1.557 nM Compound: Osimertinib	Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
A549	IC₅₀	9.4 μM Compound: OSI	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
A549	IC₅₀	1.44 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38142512]
A549	IC₅₀	1.661 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 38169271]
A549	IC₅₀	1.23 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
A549	IC₅₀	1.87 μM Compound: Osimertinib	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38879996]
A549	IC₅₀	0.86 μM Compound: Osimertinib	Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 39094428]
ASPC1	IC₅₀	3.985 μM Compound: 6; AZD-9291	Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay	[PMID: 30471829]
BaF3	IC₅₀	>1 μM Compound: 65, AZD9291	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	GI₅₀	1.2 μM Compound: 5; AZD9291	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
BaF3	IC₅₀	752.4 nM Compound: Osimertinib	Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
BaF3	EC₅₀	16 nM Compound: Osimertinib	Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	1748 nM Compound: Osimertinib	Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	18 nM Compound: Osimertinib	Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	20 nM Compound: Osimertinib	Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	6 nM Compound: Osimertinib	Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	66 nM Compound: Osimertinib	Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	>5000 nM Compound: Osimertinib	Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	4.61 μM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	5.15 μM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	3.93 μM Compound: 4; AZD9291	Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	5.11 μM Compound: 4; AZD9291	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	1 nM Compound: Osimertinib	Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	1100 nM Compound: Osimertinib	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	3100 nM Compound: Osimertinib	Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay	[PMID: 31689114]
BaF3	IC₅₀	780 nM Compound: Osimertinib	Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	81 nM Compound: Osimertinib	Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	5.47 μM Compound: 6, AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay	[PMID: 32631532]
BaF3	IC₅₀	21.5 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay	[PMID: 33459024]
BaF3	IC₅₀	4 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay	[PMID: 33459024]
BaF3	IC₅₀	>3000 nM Compound: 4	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34464874]
BaF3	IC₅₀	110 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	1200 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	16 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	2 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	3 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	3.3 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	8 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	800 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	2.885 μM Compound: AZD9291; 5	Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	2.893 μM Compound: AZD9291; 5	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	4.427 μM Compound: AZD9291; 5	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	3.52 μM Compound: 5	Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	4.27 μM Compound: 5	Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	6.071 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 35446588]
BaF3	EC₅₀	0.545 μM Compound: Osimertinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	GI₅₀	0.347 μM Compound: Osimertinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	IC₅₀	0.033 μM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36064123]
BaF3	IC₅₀	0.859 μM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36064123]
BaF3	IC₅₀	10.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1320.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1409.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1475 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1503.9 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	154.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	2.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	300.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	4.3 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	4.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	53.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	60.6 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	3.38 μM Compound: 5	Cytotoxicity against mouse BaF3 cells harboring EGFR-Del19/T790M/C797S mutant assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against mouse BaF3 cells harboring EGFR-Del19/T790M/C797S mutant assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 36417820]
BaF3	IC₅₀	4.14 μM Compound: 5	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36417820]
BaF3	EC₅₀	14 nM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	EC₅₀	3.2 nM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	EC₅₀	34 nM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	CC₅₀	14 nM Compound: 6; AZD9291	Antiproliferative activity against mouse BaF3 cells overexpressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 96 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells overexpressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 96 hrs by MTS assay	[PMID: 36749735]
BaF3	IC₅₀	1.634 μM Compound: OSI	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
BaF3	IC₅₀	4.484 μM Compound: OSI	Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
BaF3	EC₅₀	2956 nM Compound: 1	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	EC₅₀	6 nM Compound: 1	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	GI₅₀	14 nM Compound: Osi; AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	GI₅₀	179 nM Compound: Osi; AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	GI₅₀	299 nM Compound: Osi; AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	GI₅₀	376 nM Compound: Osi; AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	IC₅₀	350.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	57 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	GI₅₀	107 nM Compound: 1	Inhibition of cell proliferation of mouse BaF3 cells expressing wild-type EGFR (unknown origin) Inhibition of cell proliferation of mouse BaF3 cells expressing wild-type EGFR (unknown origin)	[PMID: 38065292]
BaF3	GI₅₀	1288 nM Compound: 1	Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant (unknown origin) Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant (unknown origin)	[PMID: 38065292]
BaF3	GI₅₀	2065 nM Compound: 1	Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR Del19/T790M/C797S mutant (unknown origin) Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR Del19/T790M/C797S mutant (unknown origin)	[PMID: 38065292]
BaF3	IC₅₀	0.009 μM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring wildtype EGFR assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring wildtype EGFR assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
BaF3	IC₅₀	0.75 μM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR Del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR Del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
BaF3	IC₅₀	1.12 μM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
BaF3	IC₅₀	19 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR-L858R/C775S mutant assessed as inhibition of cell proliferation measured after 3 days by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR-L858R/C775S mutant assessed as inhibition of cell proliferation measured after 3 days by CellTiter-Glo assay	[PMID: 38300264]
BC	IC₅₀	0.015 μM Compound: 58; AZD9291	Inhibition of cell growth in human multiple BC cells bearing EZH2 T790M mutant Inhibition of cell growth in human multiple BC cells bearing EZH2 T790M mutant	[PMID: 35093670]
BC	IC₅₀	0.015 μM Compound: 58; AZD9291	Inhibition of cell growth in human multiple BC cells bearing wildtype EZH2 Inhibition of cell growth in human multiple BC cells bearing wildtype EZH2	[PMID: 35093670]
BEAS-2B	IC₅₀	14.9 μM Compound: 1; AZD9291	Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay	[PMID: 28716641]
BJ	IC₅₀	>10 μM Compound: AZD9291	Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
Calu-3	GI₅₀	264 nM Compound: 8	Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
Calu-3	IC₅₀	0.75 μM Compound: Osimertinib	Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
Calu-6	IC₅₀	5.86 μM Compound: Osimertinib	Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
CHO	GI₅₀	4.2 μM Compound: 5; AZD9291	Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
CL97	IC₅₀	0.1 μM Compound: Osimertinib	Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
EA.hy 926	IC₅₀	1.161 μM Compound: Osimertinib	Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
HaCaT	IC₅₀	73.7 nM Compound: 5; AZD9291	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method	[PMID: 27433829]
HaCaT	IC₅₀	3.356 μM Compound: Osi	Cytotoxicity against human HaCaT cells Cytotoxicity against human HaCaT cells	[PMID: 38908104]
HCC827	IC₅₀	61.6 nM Compound: AZD9291	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant	[PMID: 28426996]
HCC827	EC₅₀	<0.014 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	IC₅₀	0.027 μM Compound: AZD	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay	[PMID: 29466773]
HCC827	IC₅₀	25.4 nM Compound: AZD9291	Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay	[PMID: 29576272]
HCC827	IC₅₀	0.027 μM Compound: osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay	[PMID: 29853340]
HCC827	IC₅₀	0.011 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay	[PMID: 30442506]
HCC827	IC₅₀	0.003 μM Compound: 4	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
HCC827	IC₅₀	0.2 μM Compound: AZD9291	Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 31889606]
HCC827	IC₅₀	0.036 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
HCC827	IC₅₀	0.97 nM Compound: AZD9291	Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
HCC827	IC₅₀	0.00173 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay	[PMID: 34794818]
HCC827	IC₅₀	1 nM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
HCC827	IC₅₀	0.00248 μM Compound: Osimertinib	Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
HCC827	IC₅₀	0.004 μM Compound: Osimertinib	Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
HCC827	IC₅₀	0.003 μM Compound: 6	Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]
HCC827	IC₅₀	0.001 μM Compound: 5; AZD9291	Antiproliferative activity against human HCC827 cells by MTT assay Antiproliferative activity against human HCC827 cells by MTT assay	[PMID: 37336419]
HCC827	IC₅₀	32.31 nM Compound: AZD9291	Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 37356356]
HCC827	IC₅₀	33.7 nM Compound: AZD9291	Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 37356356]
HCC827	GI₅₀	4.5 nM Compound: Osi; AZD9291	Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
HCC827	IC₅₀	0.001 μM Compound: 2	Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37839342]
HCC827	IC₅₀	0.057 μM Compound: OS	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 37870244]
HCC827	IC₅₀	0.03 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 38169271]
HCC827	IC₅₀	0.006 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
HCC827	IC₅₀	0.016 μM Compound: AZD9291	Cytotoxicity against human HCC827 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human HCC827 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
HCC827	IC₅₀	0.007 μM Compound: Osimertinib	Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 39094428]
HEK293	IC₅₀	0.57 μM Compound: AZD9291	Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis	[PMID: 28426996]
HEK293-A	IC₅₀	2.418 μM Compound: AZD9291	Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
HeLa	IC₅₀	0.975 μM Compound: 3; AZD9291	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31683104]
HeLa	IC₅₀	1.83 μM Compound: AZD9291	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
HepG2	IC₅₀	1.605 μM Compound: 6; AZD9291	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 30530173]
HepG2	IC₅₀	3.06 μM Compound: 2	Antiproliferative activity against human HepG2 cells harboring VEGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells harboring VEGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37839342]
HK-2	IC₅₀	3.565 μM Compound: AZD9291	Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
HK-2	IC₅₀	2.719 μM Compound: AZD9291	Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay	[PMID: 33429247]
HK-2	IC₅₀	2.399 μM Compound: Osimertinib	Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
HK-2	IC₅₀	2.138 μM Compound: Osi	Cytotoxicity against human HK-2 cells Cytotoxicity against human HK-2 cells	[PMID: 38908104]
HT-29	IC₅₀	0.65 μM Compound: AZD9291	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 29486953]
HUVEC	IC₅₀	7.278 μM Compound: AZD9291	Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 32619886]
HUVEC	IC₅₀	2.399 μM Compound: Osi	Cytotoxicity against human HUVEC cells Cytotoxicity against human HUVEC cells	[PMID: 38908104]
HUVEC	IC₅₀	2.399 μM Compound: Osi	Cytotoxicity against VEGF-stimulated human HUVEC cells Cytotoxicity against VEGF-stimulated human HUVEC cells	[PMID: 38908104]
KG-1	IC₅₀	0.53 μM Compound: Osimertinib	Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay	[PMID: 32961382]
L02	IC₅₀	1.602 μM Compound: AZD9291	Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
L02	IC₅₀	0.3 μM Compound: AZD9291	Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 31889606]
L02	IC₅₀	>50 μM Compound: AZD9291	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
L02	IC₅₀	1.975 μM Compound: AZD9291	Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay	[PMID: 33429247]
L02	IC₅₀	>40 μM Compound: Osimertinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33640672]
L02	IC₅₀	8.42 μM Compound: Osimertinib	Cytotoxicity against human L02 cells assessed as inhibition of cell viability measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell viability measured after 72 hrs by MTT assay	[PMID: 38169271]
L02	IC₅₀	1.955 μM Compound: Osi	Cytotoxicity against human L02 cells Cytotoxicity against human L02 cells	[PMID: 38908104]
LoVo	IC₅₀	480 μM Compound: 8	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay	[PMID: 25271963]
LoVo	IC₅₀	480 nM Compound: AZD9291	Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA	[PMID: 26968253]
LoVo	IC₅₀	480 nM Compound: Osimertinib	Antiproliferative activity against human LoVo cells harboring wild-type EGFR assessed as reduction in cell viability Antiproliferative activity against human LoVo cells harboring wild-type EGFR assessed as reduction in cell viability	[PMID: 38879996]
Lymphoma cell line	IC₅₀	0.015 μM Compound: 58; AZD9291	Inhibition of cell growth in human Lymphoma cell line bearing EZH2 T790M mutant Inhibition of cell growth in human Lymphoma cell line bearing EZH2 T790M mutant	[PMID: 35093670]
Lymphoma cell line	IC₅₀	0.015 μM Compound: 58; AZD9291	Inhibition of cell growth in human Lymphoma cell line bearing wildtype EZH2 Inhibition of cell growth in human Lymphoma cell line bearing wildtype EZH2	[PMID: 35093670]
MCF7	IC₅₀	3.67 μM Compound: AZD9291	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
MCF7	IC₅₀	1.16 μM Compound: Osimertinib	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 38323982]
MCF7	IC₅₀	3.525 μM Compound: AZD9291	Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
MDA-MB-231	IC₅₀	2.25 μM Compound: AZD9291	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36762554]
MDA-MB-468	IC₅₀	1.3 μM Compound: Osimertinib	Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay	[PMID: 32961382]
NCI-H1299	IC₅₀	2.84 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay	[PMID: 34794818]
NCI-H1299	IC₅₀	>10 μM Compound: AZD9291; 5	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay	[PMID: 35178175]
NCI-H1299	IC₅₀	3.24 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
NCI-H1975	GI₅₀	24 nM Compound: 8	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	15 μM Compound: 8	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	15 μM Compound: 8	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	15 nM Compound: 9; AZD9291	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
NCI-H1975	IC₅₀	0.052 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay	[PMID: 27131639]
NCI-H1975	IC₅₀	0.03 μM Compound: 3	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 28033579]
NCI-H1975	IC₅₀	67 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant	[PMID: 28426996]
NCI-H1975	EC₅₀	0.019 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
NCI-H1975	IC₅₀	10.5 nM Compound: 1; AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 28716641]
NCI-H1975	EC₅₀	<0.014 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	0.064 μM Compound: 3; AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay	[PMID: 28987609]
NCI-H1975	IC₅₀	0.019 μM Compound: AZD	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29466773]
NCI-H1975	IC₅₀	0.06 μM Compound: AZD9291	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29486953]
NCI-H1975	IC₅₀	0.023 μM Compound: AZD-9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 29534926]
NCI-H1975	IC₅₀	47.2 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 29576272]
NCI-H1975	IC₅₀	0.041 μM Compound: 5; AZD9291	Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay	[PMID: 29730192]
NCI-H1975	IC₅₀	0.019 μM Compound: osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29853340]
NCI-H1975	IC₅₀	0.013 μM Compound: 2	Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay	[PMID: 30108918]
NCI-H1975	IC₅₀	0.13 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
NCI-H1975	GI₅₀	2.8 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay	[PMID: 30442506]
NCI-H1975	IC₅₀	0.06 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay	[PMID: 30442506]
NCI-H1975	IC₅₀	0.096 μM Compound: 6; AZD-9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay	[PMID: 30471829]
NCI-H1975	IC₅₀	0.1 μM Compound: 4	Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 30472599]
NCI-H1975	IC₅₀	0.073 μM Compound: 6; AZD9291	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 30530173]
NCI-H1975	IC₅₀	0.03 μM Compound: 4; AZD9291	Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay	[PMID: 31223440]
NCI-H1975	IC₅₀	0.05 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
NCI-H1975	IC₅₀	0.014 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
NCI-H1975	IC₅₀	0.073 μM Compound: 3; AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31683104]
NCI-H1975	IC₅₀	0.07 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	3.1 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	0.012 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
NCI-H1975	IC₅₀	<1 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
NCI-H1975	IC₅₀	0.044 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
NCI-H1975	IC₅₀	0.016 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay	[PMID: 32550993]
NCI-H1975	IC₅₀	0.74 μM Compound: 6, AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay	[PMID: 32631532]
NCI-H1975	IC₅₀	73.4 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay	[PMID: 32679450]
NCI-H1975	IC₅₀	42 nM Compound: AZD9291	Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
NCI-H1975	IC₅₀	0.011 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay	[PMID: 33429247]
NCI-H1975	IC₅₀	47.3 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay	[PMID: 33459024]
NCI-H1975	IC₅₀	0.98 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33640672]
NCI-H1975	IC₅₀	2.08 μM Compound: Osimertinib	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay	[PMID: 33640672]
NCI-H1975	IC₅₀	18.21 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay	[PMID: 33667898]
NCI-H1975	IC₅₀	0.091 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34218082]
NCI-H1975	IC₅₀	0.076 μM Compound: AZD9291	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay	[PMID: 34534838]
NCI-H1975	IC₅₀	0.0148 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay	[PMID: 34794818]
NCI-H1975	IC₅₀	0.1 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 35178185]
NCI-H1975	IC₅₀	15 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation	[PMID: 35254067]
NCI-H1975	IC₅₀	17 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
NCI-H1975	IC₅₀	0.0305 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
NCI-H1975	IC₅₀	0.072 μM Compound: 3	Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]
NCI-H1975	IC₅₀	0.125 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36173763]
NCI-H1975	IC₅₀	3.85 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36173763]
NCI-H1975	IC₅₀	4.32 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36173763]
NCI-H1975	IC₅₀	0.095 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 36288657]
NCI-H1975	IC₅₀	0.04 μM Compound: Osimertinib	Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 36375337]
NCI-H1975	CC₅₀	43 nM Compound: 6; AZD9291	Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay	[PMID: 36749735]
NCI-H1975	IC₅₀	1.3 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36762554]
NCI-H1975	IC₅₀	0.015 μM Compound: 6	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]
NCI-H1975	IC₅₀	0.019 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
NCI-H1975	IC₅₀	0.022 μM Compound: OSI	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
NCI-H1975	IC₅₀	0.13 μM Compound: 5; AZD9291	Antiproliferative activity against human NCI-H1975 cells by MTT assay Antiproliferative activity against human NCI-H1975 cells by MTT assay	[PMID: 37336419]
NCI-H1975	IC₅₀	43.63 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay	[PMID: 37356356]
NCI-H1975	IC₅₀	44.61 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay	[PMID: 37356356]
NCI-H1975	GI₅₀	35 nM Compound: Osi; AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
NCI-H1975	IC₅₀	0.03 μM Compound: 2	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37839342]
NCI-H1975	IC₅₀	0.11 μM Compound: OS	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 37870244]
NCI-H1975	IC₅₀	4.69 μM Compound: OS	Antiproliferative activity against human Osimertinib-resistant NCI-H1975 cell incubated for 72 hrs by MTT assay Antiproliferative activity against human Osimertinib-resistant NCI-H1975 cell incubated for 72 hrs by MTT assay	[PMID: 37870244]
NCI-H1975	IC₅₀	0.007 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 37885208]
NCI-H1975	IC₅₀	3 μM Compound: 17	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability	[PMID: 38043489]
NCI-H1975	IC₅₀	0.32 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38142512]
NCI-H1975	IC₅₀	2.94 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38142512]
NCI-H1975	IC₅₀	0.081 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 38169271]
NCI-H1975	IC₅₀	0.015 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 38323982]
NCI-H1975	IC₅₀	1.51 μM Compound: 7	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38401457]
NCI-H1975	IC₅₀	0.63 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
NCI-H1975	IC₅₀	2327 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cell assessed as cell growth inhibition Antiproliferative activity against human NCI-H1975 cell assessed as cell growth inhibition	[PMID: 38838547]
NCI-H1975	IC₅₀	0.004 μM Compound: Osimertinib	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 38879996]
NCI-H1975	IC₅₀	15 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38879996]
NCI-H1975	IC₅₀	18.21 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo assay	[PMID: 38879996]
NCI-H1975	IC₅₀	0.022 μM Compound: AZD9291	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
NCI-H292	IC₅₀	1.084 μM Compound: AZD9291	Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
NCI-H292	IC₅₀	0.22 μM Compound: 1	Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay	[PMID: 32550993]
NCI-H292	IC₅₀	0.924 nM Compound: AZD9291	Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay	[PMID: 33429247]
NCI-H292	IC₅₀	2 μM Compound: Osimertinib	Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 38879996]
NCI-H460	IC₅₀	415.9 nM Compound: 1; AZD9291	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay	[PMID: 28716641]
Non-small cell lung cancer cell line	IC₅₀	41 nM Compound: Osimertinib	Antiproliferative activity against Non-small cell lung cancer cells (unknown origin) Antiproliferative activity against Non-small cell lung cancer cells (unknown origin)	[PMID: 38432059]
PC-9	GI₅₀	23 nM Compound: 8	Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
PC-9	IC₅₀	17 μM Compound: 8	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
PC-9	IC₅₀	56 nM Compound: 9; AZD9291	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
PC-9	IC₅₀	17 nM Compound: AZD9291	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA	[PMID: 26968253]
PC-9	IC₅₀	11.31 nM Compound: Osimertinib	Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
PC-9	IC₅₀	3461 nM Compound: Osimertinib	Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
PC-9	IC₅₀	7.463 nM Compound: Osimertinib	Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
PC-9	IC₅₀	6.5 nM Compound: 1; AZD9291	Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay	[PMID: 28716641]
PC-9	IC₅₀	0.16 μM Compound: Osimertinib	Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay	[PMID: 30442506]
PC-9	IC₅₀	<0.01 μM Compound: Osimertinib	Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
PC-9	IC₅₀	0.016 μM Compound: AZD9291	Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
PC-9	IC₅₀	>1000 nM Compound: Osimertinib	Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
PC-9	IC₅₀	0.011 nM Compound: AZD9291	Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay	[PMID: 33429247]
PC-9	IC₅₀	0.011 μM Compound: AZD9291; 5	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	3.21 μM Compound: AZD9291; 5	Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	17 nM Compound: Osimertinib	Antiproliferative activity against human PC-9 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation Antiproliferative activity against human PC-9 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation	[PMID: 35254067]
PC-9	IC₅₀	5.431 nM Compound: 5	Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
PC-9	IC₅₀	3.248 μM Compound: AZD9291	Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
PC-9	IC₅₀	0.08 μM Compound: 5	Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 36417820]
PC-9	IC₅₀	4.85 μM Compound: 5	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36417820]
PC-9	IC₅₀	0.023 nM Compound: Osimertinib	Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
PC-9	IC₅₀	0.021 μM Compound: OSI	Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
PC-9	GI₅₀	6.7 nM Compound: Osi; AZD9291	Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
PC-9	IC₅₀	0.005 μM Compound: Osimertinib	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 37885208]
PC-9	IC₅₀	2.2 μM Compound: Osimertinib	Antiproliferative activity against human PC-9 cells harbouring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells harbouring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 37885208]
PC-9	IC₅₀	0.005 μM Compound: Osimertinib	Cytotoxicity against human PC-9 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity against human PC-9 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 38879996]
PC-9	IC₅₀	17 nM Compound: Osimertinib	Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 38879996]
PC-9	IC₅₀	0.015 μM Compound: AZD9291	Cytotoxicity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
PC-9	IC₅₀	2.789 μM Compound: AZD9291	Cytotoxicity against human PC-9 cells expressing EGFR Del19/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human PC-9 cells expressing EGFR Del19/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
PC-9	IC₅₀	3.248 μM Compound: AZD9291	Cytotoxicity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
Sf9	IC₅₀	20.8 nM Compound: 6; AZD-9291	Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay	[PMID: 30471829]
Sf9	IC₅₀	567.5 nM Compound: 6; AZD-9291	Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay	[PMID: 30471829]
Sf9	IC₅₀	0.002 μM Compound: Osimertinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k	[PMID: 31718182]
Sf9	IC₅₀	0.09 μM Compound: Osimertinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki	[PMID: 31718182]
Sf9	IC₅₀	1.23 μM Compound: Osimertinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay	[PMID: 31718182]
U-87MG ATCC	IC₅₀	4.5 μM Compound: 4	Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
Vero	CC₅₀	13.23 μM Compound: Osimertinib	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	3.26 μM Compound: Osimertinib	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC₅₀s of 41, 26, 41, and 31 nM, respectively^[2].
? Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC₅₀s of 6, 7, and 74 nM, respectively^[2].
? Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC₅₀ ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)^[2].
? Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC₅₀ of 8 nM in PC-9) and T790M (mean IC₅₀s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC₅₀s of 650 and 461 nM in Calu3 and H2073 respectively)^[1].
? Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) ^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration:

0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

72 hours
Result:

Inhibited cell proliferation (IC₅₀s=6, 7, 74 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:

PC-9, H3255, PC-9ER, and H1975 cells
Concentration:

0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

72 hours
Result:

Dramatically inhibited cell proliferation (IC₅₀s=41, 26, 41, 31 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:

Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
Concentration:

0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

72 hours
Result:

Inhibited cell proliferation (IC₅₀s=16, 701, 230, 38 nM, respectively)

Apoptosis Analysis^[2]

Cell Line:

Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
Concentration:

0.1 μM
Incubation Time:

48 hours
Result:

Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.

In Vivo

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models^[1]
Dosage:

0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration:

p.o.; daily for 14 days
Result:

Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1421373-65-0
Appearance Solid
Masse moléculaire 499.61
Formule C₂₈H₃₃N₇O₂
Color Light yellow to brown
SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
Synonyms

AZD-9291; Mereletinib
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (202)

All WBCell Proliferation/Viability AssayIF

Sort by:

Journal Impact Factor

Signal Transduct Target Ther

MUCIN 1 confers inflammatory memory of tyrosine kinase inhibitor resistance in non-small cell lung cancer. [Abstract]

2025 Nov 28;10(1):389. PMID: 41309558
Science

A genetically encoded device for transcriptome storage in mammalian cells. [Abstract]

2026 Mar 26;391(6792):eadz9353. PMID: 41538410
Cancer Cell

A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]

2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213
Cancer Cell

Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway. [Abstract]

2020 Jan 13;37(1):104-122.e12. PMID: 31935369
Eur Heart J

Osimertinib induces reversible cardiac dysfunction through the GATA4-MYLK3-MYL2 axis. [Abstract]

2025 Dec 3:ehaf813. PMID: 41330421
Cancer Discov

Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. [Abstract]

2019 Jul;9(7):926-943. PMID: 31092401
Nat Cancer

Scribble mis-localization induces adaptive resistance to KRAS G12C inhibitors through feedback activation of MAPK signaling mediated by YAP-induced MRAS. [Abstract]

2023 Jun;4(6):829-843. PMID: 37277529

Osimertinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]

HCC827 (EGFR mutant) and NCI-H2228 (ALK-translocated) lung cancer cells were treated with 100 nM of the EGFR inhibitor Osimertinib or 500 nM of the ALK inhibitor alectinib for 72 h, respectively. Representative immunofluorescence images of E-cadherin were merged with DAPI. Scale bar, 10 μm.

Osimertinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]

HCC827 and NCI-H2228 cancer cell lines were treated with 100 nM Osimertinib, 500 nM alectinib or 50 nM trametinib for 72 h as indicated. Immunofluorescence images of Scrib were merged with DAPI. Scale bar, 10 μm.

Osimertinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]

Osimertinib-induced MRAS activation was abrogated by the addition of either SHP2 or SOS1 inhibitor in HCC827 cells. HCC827 cells were treated with 100 nM Osimertinib with or without 10 μM BI-3406 or 10 μM SHP099 for 72 h.
Nat Cancer

An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. [Abstract]

2022 Apr;3(4):402-417. PMID: 35422503
Adv Mater

Highly Specific Cytokine Receptor-Targeting Chimeras for Targeted Membrane Protein Degradation and Sensitization of Osimertinib in EGFR-Mutated Non-Small-Cell Lung Cancer. [Abstract]

2025 May 22:e2504050. PMID: 40401615
Drug Resist Updat

Stabilin-1+ lipid-associated macrophages promote lung adenocarcinoma liver metastasis and osimertinib resistance through impairing macrophage phagocytosis via SIRPα-CD47 axis. [Abstract]

2026 May:86:101379. PMID: 41719890
Cancer Res

Enozertinib is a Selective, Brain-penetrant EGFR inhibitor for Treating Non-small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations. [Abstract]

2025 Nov 6. PMID: 41196054
Mol Cell

Amplified dosage of the NKX2-1 lineage transcription factor controls its oncogenic role in lung adenocarcinoma. [Abstract]

2025 Mar 21:S1097-2765(25)00194-7. PMID: 40139189
Cancer Res

Loss of CDKN2A Enhances the Efficacy of Immunotherapy in EGFR-Mutant Non-Small Cell Lung Cancer. [Abstract]

2025 Feb 1;85(3):585-601. PMID: 39514336
Cancer Res

Osimertinib covalently binds to CD34 and eliminates myeloid leukemia stem/progenitor cells. [Abstract]

2024 Feb 1;84(3):479-492. PMID: 38095536
Cancer Res

RBM10 Loss Promotes EGFR-Driven Lung Cancer and Confers Sensitivity to Spliceosome Inhibition. [Abstract]

2023 May 2;83(9):1490-1502. PMID: 36853175
Cancer Res

Metabolic reprogramming driven by IGF2BP3 promotes acquired resistance to EGFR inhibitors in non-small cell lung cancer. [Abstract]

2023 Jul 5;83(13):2187-2207. PMID: 37061993
ACS Nano

An Osimertinib-Perfluorocarbon Nanoemulsion with Excellent Targeted Therapeutic Efficacy in Non-small Cell Lung Cancer: Achieving Intratracheal and Intravenous Administration. [Abstract]

2022 Aug 23;16(8):12590-12605. PMID: 35863049
Nat Commun

B7-H3-mediated cis-inhibition of EGFR by a tumor-selective bispecific antibody enhances anti-tumor efficacy and minimizes toxicities. [Abstract]

2026 Feb 24;17(1):3113. PMID: 41735305
Nat Commun

An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]

2026 Jan 21;17(1):1902. PMID: 41565660
Cell Death Differ

PD-L2 drives resistance to EGFR-TKIs: dynamic changes of the tumor immune environment and targeted therapy. [Abstract]

2024 Sep;31(9):1140-1156. PMID: 38816578
Adv Sci (Weinh)

CauFinder: Steering Cell-State and Phenotype Transitions by Causal Disentanglement Learning. [Abstract]

2026 Jun 16:e76177. PMID: 42301228
Adv Sci (Weinh)

Splicing Shift of RAC1 Accelerates Tumorigenesis and Defines a Potent Therapeutic Target in Lung Cancer. [Abstract]

2025 Jun 23:e03322. PMID: 40548642
Adv Sci (Weinh)

Addressing Clinical Limitations of Glutaminase Inhibitors: Novel Strategies for Osimertinib-Resistant Lung Cancer by Exploiting Glutamine Metabolic Dependency. [Abstract]

2024 Dec 16:e2411479. PMID: 39680480
Adv Sci (Weinh)

Brain Metastasis from EGFR-Mutated Non-Small Cell Lung Cancer: Secretion of IL11 from Astrocytes Up-Regulates PDL1 and Promotes Immune Escape. [Abstract]

2024 Jul;11(26):e2306348. PMID: 38696655
Exp Hematol Oncol

Combined inhibition of MET and VEGF enhances therapeutic efficacy of EGFR TKIs in EGFR-mutant non-small cell lung cancer with concomitant aberrant MET activation. [Abstract]

2024 Oct 1;13(1):97. PMID: 39354638
Theranostics

Endogenous glutamate determines ferroptosis sensitivity via ADCY10-dependent YAP suppression in lung adenocarcinoma. [Abstract]

2021 Mar 24;11(12):5650-5674. PMID: 33897873
Theranostics

ILT4 inhibition prevents TAM- and dysfunctional T cell-mediated immunosuppression and enhances the efficacy of anti-PD-L1 therapy in NSCLC with EGFR activation. [Abstract]

2021 Jan 19;11(7):3392-3416. PMID: 33537094
J Exp Clin Cancer Res

Hypoxia-inducible APCDD1L-AS1 promotes osimertinib resistance by stabilising DLST to drive tricarboxylic acid cycle in lung adenocarcinoma. [Abstract]

2025 Jul 9;44(1):197. PMID: 40634956
J Exp Clin Cancer Res

RBM10 deficiency promotes brain metastasis by modulating sphingolipid metabolism in a BBB model of EGFR mutant lung adenocarcinoma. [Abstract]

2025 Mar 11;44(1):95. PMID: 40069781
J Exp Clin Cancer Res

The third-generation EGFR inhibitor AZD9291 overcomes primary resistance by continuously blocking ERK signaling in glioblastoma. [Abstract]

2019 May 23;38(1):219. PMID: 31122294

Osimertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]

Measurement of antiproliferation effects of AZD9291 (Osimertinib) (0.5-2 μM; 24 h) by EdU incorporation assay.

Osimertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]

U87 and U251 cells are exposed to indicated concentrations of AZD9291 (Osimertinib) for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.

Osimertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]

U87 and U251 cells are treated with AZD9291 (Osimertinib) or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.

Osimertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]

GBM cells were treated by different concentrations of AZD9291 (Osimertinib) (0.625–20 μM) for 72 h. The cell viability was examined by CCK8 assay. Comparation of different sensitive of GBM cells to EGFR inhibitors (AZD9291, Erlotinib and Gefitinib).
J Exp Clin Cancer Res

Co-administration of 20(S)-protopanaxatriol (g-PPT) and EGFR-TKI overcomes EGFR-TKI resistance by decreasing SCD1 induced lipid accumulation in non-small cell lung cancer. [Abstract]

2019 Mar 15;38(1):129. PMID: 30876460
Sci Adv

A genome-wide genetic screen reveals the P2Y2-integrin axis as a stabilizer of EGFR mutants in non-small cell lung cancer (NSCLC). [Abstract]

2026 Jan 23;12(4):eadv3980. PMID: 41564171
Sci Adv

Targeting RRM2 with dual-modal theranostic smart nanoresponder overcomes osimertinib resistance and triggers immune remodeling in NSCLC. [Abstract]

2025 Oct 17;11(42):eady7930. PMID: 41105786
Redox Biol

C-terminal interleukin 1 alpha (IL-1α) overexpression drives EMT and a vulnerability to ferroptosis in HNSCC. [Abstract]

2026 Jun:93:104172. PMID: 42013543
J Control Release

Macropinocytosis-targeted peptide-docetaxel conjugate for bystander pancreatic cancer treatment. [Abstract]

2024 Dec:376:829-841. PMID: 39491626
Cell Rep Med

Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse. [Abstract]

2024 Mar 19;5(3):101471. PMID: 38508142
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Clin Cancer Res

STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models. [Abstract]

2025 Jun 4:OF1-OF17. PMID: 40465424
Cancer Lett

Identification and characterization of Bufalin as a novel EGFR degrader. [Abstract]

2025 Apr 10:217715. PMID: 40220852
Cancer Lett

A novel EGFR inhibitor acts as potent tool for hypoxia-activated prodrug systems and exerts strong synergistic activity with VEGFR inhibition in vitro and in vivo. [Abstract]

2023 Jul 1:565:216237. PMID: 37211067
Int J Biol Sci

MUC3A induces PD-L1 and reduces tyrosine kinase inhibitors effects in EGFR-mutant non-small cell lung cancer. [Abstract]

2021 Apr 12;17(7):1671-1681. PMID: 33994852
Cell Death Dis

Cancer-associated fibroblasts promote osimertinib resistance in non-small cell lung cancer cells via METTL1-mediated NET1 m7G modification. [Abstract]

2026 Feb 21;17(1):248. PMID: 41723107
Cell Death Dis

Integrative multi-omics identifies AP-1 transcription factor as a targetable mediator of acquired osimertinib resistance in non-small cell lung cancer. [Abstract]

2025 May 25;16(1):414. PMID: 40414926
Cell Death Dis

MCT1 relieves osimertinib-induced CRC suppression by promoting autophagy through the LKB1/AMPK signaling. [Abstract]

2019 Aug 13;10(8):615. PMID: 31409796
Cell Death Dis

AXL degradation in combination with EGFR-TKI can delay and overcome acquired resistance in human non-small cell lung cancer cells. [Abstract]

2019 May 1;10(5):361. PMID: 31043587
Genes Dis

2026 Feb 28.
J Pharm Anal

2026 Jun 3.
J Pharm Anal

Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells. [Abstract]

2021 Dec;11(6):799-807. PMID: 35028186
Dev Cell

Stress-induced pro-inflammatory glioblastoma stem cells secrete TNFAIP6 to enhance tumor growth and induce suppressive macrophages. [Abstract]

2025 May 15:S1534-5807(25)00287-4. PMID: 40403724
Int J Biol Macromol

Exploring the association of POSTN+ cancer-associated fibroblasts with triple-negative breast cancer. [Abstract]

2024 May;268(Pt 1):131560. PMID: 38631570
Acta Pharmacol Sin

Ivacaftor, a CFTR potentiator, synergizes with osimertinib against acquired resistance to osimertinib in NSCLC by regulating CFTR-PTEN-AKT axis. [Abstract]

2025 Apr;46(4):1045-1057. PMID: 39627385
Acta Pharmacol Sin

Targeting DNA-PK overcomes acquired resistance to third-generation EGFR-TKI osimertinib in non-small-cell lung cancer. [Abstract]

2021 Apr;42(4):648-654. PMID: 33414509
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Acta Pharmacol Sin

AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition. [Abstract]

2019 Dec;40(12):1587-1595. PMID: 31171828

Osimertinib purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595. [Abstract]

MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly
Phytomedicine

Halofuginone targets Serine/Glycine synthesis to reverse epidermal growth factor receptor Tyrosine Kinase inhibitor resistance in lung adenocarcinoma. [Abstract]

2025 Jul 25:143:156788. PMID: 40354707
Free Radic Biol Med

Targeting PDK4 to mitigate osimertinib-induced cardiotoxicity: Insights into mitochondria-endoplasmic reticulum crosstalk and necroptosis. [Abstract]

2025 Aug 9:240:267-283. PMID: 40789497
NPJ Precis Oncol

High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]

2026 Apr 8;10(1):211. PMID: 41951768
NPJ Precis Oncol

GLMP promotes EGFR-TKI resistance by activating autophagy and RhoA pathway in non-small cell lung cancer. [Abstract]

2025 Nov 26;9(1):391. PMID: 41298761
Neoplasia

The antitumor activity of osimertinib plus palbociclib in non-small cell lung cancer patient-derived xenograft (PDX)/2D/3D culture models harboring EGFR amplification and CDKN2A/2B homozygous deletions. [Abstract]

2024 Aug 14:57:101039. PMID: 39146623
Biomed Pharmacother

Therapeutic strategy using novel RET/YES1 dual-target inhibitor in lung cancer. [Abstract]

2024 Feb:171:116124. PMID: 38198957
Oncogene

Amphiregulin drives EGFR-dependent genome stability in colorectal cancer and represents a targetable vulnerability. [Abstract]

2026 Jun 15. PMID: 42298179
Oncogene

YTHDC2 inhibits the resistance of lung cancer to EGFR-TKI through cuproptosis. [Abstract]

2025 Dec 16. PMID: 41402633
Stem Cell Res Ther

L-Glutamate enables the EGFR-MEK-ERK-mTFB2 axis to enhance mitochondrial biogenesis in intestinal stem cells. [Abstract]

2025 Oct 31;16(1):599. PMID: 41174788
Oncogene

Cancer-associated fibroblasts promote EGFR-TKI resistance via the CTHRC1/glycolysis/H3K18la positive feedback loop. [Abstract]

2025 May;44(19):1400-1414. PMID: 40011576
Oncogene

NEU4-mediated desialylation enhances the activation of the oncogenic receptors for the dissemination of ovarian carcinoma. [Abstract]

2024 Nov;43(49):3556-3569. PMID: 39402373
Oncogene

PrPC controls epithelial-to-mesenchymal transition in EGFR-mutated NSCLC: implications for TKI resistance and patient follow-up. [Abstract]

2024 Sep;43(37):2781-2794. PMID: 39147880
Oncogene

CRL2KLHDC3 mediates p14ARF N-terminal ubiquitylation degradation to promote non-small cell lung carcinoma progression. [Abstract]

2022 May;41(22):3104-3117. PMID: 35468939
Cell Chem Biol

Systematic cysteine scanning identifies a druggable pocket in oncogenic KRAS. [Abstract]

2026 Feb 11:S2451-9456(26)00027-9. PMID: 41679298
J Natl Cancer Inst

Suppressing c-FOS expression by G-quadruplex ligands inhibits osimertinib-resistant non-small cell lung cancers. [Abstract]

2023 Nov 8;115(11):1383-1391. PMID: 37481710
Cell Chem Biol

Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation. [Abstract]

2018 Aug 16;25(8):996-1005.e4. PMID: 29909991

Osimertinib purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. [Abstract]

Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.
Cell Rep

circATF6 triggers calcium overload to synergize with EGFR-TKI in non-small cell lung cancer via modulation of proteostasis. [Abstract]

2025 Dec 5;44(12):116659. PMID: 41351835
Cell Rep

A MYC-STAMBPL1-TOE1 positive feedback loop mediates EGFR stability in hepatocellular carcinoma. [Abstract]

2024 Oct 8;43(10):114812. PMID: 39388352
Appl Surf Sci

2024 Dec 21.
J Med Chem

Don't Lose Your (War)head: Structure-Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation. [Abstract]

2026 May 14;69(9):11574-11591. PMID: 42062179
J Med Chem

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. [Abstract]

2025 Aug 28;68(16):17917-17932. PMID: 40801664
J Med Chem

Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1. [Abstract]

2023 Apr 27;66(8):5427-5438. PMID: 37040446
J Med Chem

Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. [Abstract]

2017 Apr 13;60(7):2944-2962. PMID: 28282122
Int J Nanomedicine

A Hybrid Protein-Oxygen Nanomedicine Overcomes Osimertinib Resistance in NSCLC via HIF-1α/VEGF/EGFR Inhibition. [Abstract]

2025 Aug 27:20:10389-10405. PMID: 40901248
Ecotoxicol Environ Saf

PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]

2025 Nov 15:307:119433. PMID: 41273832
Cancer Cell Int

SHP2 inhibition enhances the anticancer effect of Osimertinib in EGFR T790M mutant lung adenocarcinoma by blocking CXCL8 loop mediated stemness. [Abstract]

2021 Jul 3;21(1):337. PMID: 34217295
Cancer Cell Int

Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma. [Abstract]

2021 Apr 15;21(1):216. PMID: 33858423
Int J Mol Med

Suppression of tumor growth by GMI, an edible fungal immunomodulatory protein, is associated with targeting GSK3β‑mediated proteasomal degradation of PD‑L1. [Abstract]

2025 Dec;56(6):217. PMID: 41070618
Int J Mol Med

Characterization of circRNAs in established osimertinib‑resistant non‑small cell lung cancer cell lines. [Abstract]

2023 Nov;52(5):102. PMID: 37681495
Heart Rhythm

Osimertinib induces prolongation of action potential duration via downregulation of KCNN1 expression: Exploring the potential mechanisms of arrhythmia. [Abstract]

2025 Jul 11:S1547-5271(25)02640-2. PMID: 40653133
Biochem Pharmacol

Lysine methylation-mediated SMYD2 degradation by casticin sensitizes non-small-cell lung cancer cells to osimertinib therapy. [Abstract]

2026 Jan;243(Pt 2):117562. PMID: 41314435
Biochem Pharmacol

Targeting N6-methyladenosine demethylase FTO overcomes osimertinib resistance by inducing G0/G1 phase arrest in an m6A-dependent manner in lung adenocarcinoma. [Abstract]

2025 Jul 29;242(Pt 1):117198. PMID: 40744230
Pharmaceutics

Inhalable Anti-EGFR Antibody-Conjugated Osimertinib Liposomes for Non-Small Cell Lung Cancer. [Abstract]

2024 Nov 12;16(11):1444. PMID: 39598567
Mol Cancer Ther

AMT-562, a Novel HER3-targeting Antibody-Drug Conjugate, Demonstrates a Potential to Broaden Therapeutic Opportunities for HER3-expressing Tumors. [Abstract]

2023 Sep 5;22(9):1013-1027. PMID: 37302522
Drug Deliv Transl Res

Pulmonary delivery of osimertinib liposomes for non-small cell lung cancer treatment: formulation development and in vitro evaluation. [Abstract]

2022 Oct;12(10):2474-2487. PMID: 34816394
Mol Cancer Ther

TAS-121, A Selective Mutant EGFR Inhibitor, Shows Activity Against Tumors Expressing Various EGFR Mutations Including T790M and Uncommon Mutations G719X. [Abstract]

2019 May;18(5):920-928. PMID: 30872380
Mol Cancer Ther

Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury. [Abstract]

2018 Mar;17(3):603-613. PMID: 29237806
Chem Biol Interact

A microfluidic human blood-brain barrier model reveals neurovascular toxicity and barrier disruption induced by E-cigarette additives. [Abstract]

2026 Aug 1:436:112206. PMID: 42285244
J Ethnopharmacol

Taxus chinensis var. mairei (Lemée et Lévl) Cheng et L.K. Fu overcomes the resistance to osimertinib in EGFR-mutant non-small-cell lung cancer via suppression of ERK1/2-related cholesterol biosynthesis. [Abstract]

2024 Jul 18:118586. PMID: 39032664
Int J Pharm

Microfluidic-assisted preparation of ARV 825 and Osimertinib loaded liposomal formulation as a potential system for colorectal cancer therapy. [Abstract]

2025 Dec 25:686:126358. PMID: 41192598
Cancer Drug Resist

Novel FAK inhibitors suppress tumor growth and reverse EGFR-TKI resistance in non-small cell lung cancer. [Abstract]

2025 Nov 5:8:57. PMID: 41281943
Commun Biol

SNX16 aggravates AngII-induced cardiac hypertrophy in mice via EGFR transactivation. [Abstract]

2025 Nov 29. PMID: 41318855
Commun Biol

EGFR signaling and pharmacology in oncology revealed with innovative BRET-based biosensors. [Abstract]

2024 Mar 1;7(1):250. PMID: 38429428
Commun Biol

A small-molecule compound D6 overcomes EGFR-T790M-mediated resistance in non-small cell lung cancer. [Abstract]

2021 Dec 13;4(1):1391. PMID: 34903832
Respir Res

TGM2-TUFM promotes acquired resistance to EGFR-TKIs in EGFR-mutated NSCLC through p62-mediated lipophagy. [Abstract]

2026 May 9. PMID: 42106683
Respir Res

Combination of betulinic acid and EGFR-TKIs exerts synergistic anti-tumor effects against wild-type EGFR NSCLC by inducing autophagy-related cell death via EGFR signaling pathway. [Abstract]

2024 May 20;25(1):215. PMID: 38764025
Cancer Gene Ther

YAP 5-methylcytosine modification increases its mRNA stability and promotes the transcription of exosome secretion-related genes in lung adenocarcinoma. [Abstract]

2023 Jan;30(1):149-162. PMID: 36123390
Int J Mol Sci

JAC4 Inhibits EGFR-Driven Lung Adenocarcinoma Growth and Metastasis through CTBP1-Mediated JWA/AMPK/NEDD4L/EGFR Axis. [Abstract]

2023 May 15;24(10):8794. PMID: 37240137
Int J Oncol

Clinical importance of long non‑coding RNA LINC00460 expression in EGFR‑mutant lung adenocarcinoma. [Abstract]

2020 Jan;56(1):243-257. PMID: 31789388
Cell Oncol (Dordr)

Pharmacological inhibition of PGK1 suppresses EGFR-positive esophageal squamous cell carcinoma by dual targeting of glycolysis and autophagy-dependent EGFR degradation. [Abstract]

2026 Apr 29;49(3):82. PMID: 42053736
Cell Oncol (Dordr)

Proteasomal deubiquitylase activity enhances cell surface recycling of the epidermal growth factor receptor in non-small cell lung cancer. [Abstract]

2022 Oct;45(5):951-965. PMID: 36129611
Int Immunopharmacol

HMOX1 expression influence the role of macrophage in EGFR-TKI resistance of lung adenocarcinoma. [Abstract]

2026 Jan 1;168(Pt 1):115795. PMID: 41205382
Bioorg Chem

A pomalidomide-based gefitinib PROTAC degrader effectively inhibits lung cancer progression in EGFR-TKIs-acquired resistant models by targeting EGFR degradation and ETFA-mediated ATP generation. [Abstract]

2025 Aug 9:164:108864. PMID: 40815992
Mol Cancer Res

METTL14-mediated Bim mRNA m6A modification augments osimertinib sensitivity in EGFR-mutant NSCLC cells. [Abstract]

2024 Nov 1;22(11):1051-1063. PMID: 38953880
Int Immunopharmacol

Identifying the critical oncogenic mechanism of LDHA based on a prognostic model of T-cell synthetic drivers. [Abstract]

2024 Jan 5:126:111265. PMID: 38000233
Bioorg Chem

Exploration of novel dihydroquinoxalinone derivatives as EGFRL858R/T790M tyrosine kinase inhibitors for the treatment of non-small-cell lung cancer. [Abstract]

2023 Jun:135:106494. PMID: 37011522
Eur J Pharmacol

XHL11, a novel selective EGFR inhibitor, overcomes EGFRT790M-mediated resistance in non-small cell lung cancer. [Abstract]

2021 Sep 15:907:174297. PMID: 34217707
Mol Cancer Res

TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. [Abstract]

2019 Nov;17(11):2233-2243. PMID: 31467113
Mol Cancer Res

Activation of AXL as a Preclinical Acquired Resistance Mechanism Against Osimertinib Treatment in EGFR-Mutant Non-Small Cell Lung Cancer Cells. [Abstract]

2019 Feb;17(2):499-507. PMID: 30463991
Cell Rep Methods

Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]

2026 Jun 15;6(6):101339. PMID: 42134319
Mol Oncol

Nicotinamide N-methyltransferase promotes drug resistance in lung cancer, as revealed by nascent proteomic profiling. [Abstract]

2025 Jul 18. PMID: 40679940
Mol Oncol

Inhibition of CDCP1 by 8-isopentenylnaringenin synergizes with EGFR inhibitors in lung cancer treatment. [Abstract]

2023 Aug;17(8):1648-1665. PMID: 37013960
Cancers

Spironolactone, a Classic Potassium-Sparing Diuretic, Reduces Survivin Expression and Chemosensitizes Cancer Cells to Non-DNA-Damaging Anticancer Drugs. [Abstract]

2019 Oct 14;11(10):1550. PMID: 31614999
Cancers

Brexpiprazole, a Serotonin-Dopamine Activity Modulator, Can Sensitize Glioma Stem Cells to Osimertinib, a Third-Generation EGFR-TKI, via Survivin Reduction. [Abstract]

2019 Jul 5;11(7):947. PMID: 31284441
iScience

USP5-mediated CD73 deubiquitination drives osimertinib resistance via PI3K/AKT and glycolysis activation in LUAD. [Abstract]

2026 Feb 5;29(3):114916. PMID: 41767275
Antiviral Res

Repurposing screen using a robust human rhinovirus infectious clone identifies pyrvinium pamoate with antiviral activity. [Abstract]

2026 Jun:250:106417. PMID: 42025967
Adv Ther

2024 Jul 18.
J Cell Physiol

Overexpression of N-acetylglucosaminyltransferase V promotes human parotid gland acinar cell immortalization via the epidermal receptor activation. [Abstract]

2022 Mar;237(3):1780-1789. PMID: 34806177
Sci Rep

USP7-dependent stabilization of FKBP4 contributes to acquired osimertinib resistance through glycolytic remodeling in NSCLC. [Abstract]

2026 Apr 24;16(1):18984. PMID: 42031983
Sci Rep

Cysteine-reactive mitigators of small vessel disease-related NOTCH3 mutants. [Abstract]

2026 Mar 20;16(1):14300. PMID: 41862552
J Biol Chem

Diarylheptanoid 35d overcomes EGFR TKI resistance by inducing hsp70-mediated lysosomal degradation of EGFR in EGFR-mutant lung adenocarcinoma. [Abstract]

2023 Jun;299(6):104814. PMID: 37178919
Cancer Res Treat

MLL4 Regulates the Progression of Non-Small-Cell Lung Cancer by Regulating the PI3K/AKT/SOX2 Axis. [Abstract]

2023 Jul;55(3):778-803. PMID: 36701842
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Transl Lung Cancer Res

Development of a 3D-3 co-culture microbead consisting of cancer-associated fibroblasts and human umbilical vein endothelial cells for the anti-tumor drug assessment of lung cancer. [Abstract]

2025 Jun 30;14(6):2159-2179. PMID: 40673102
Transl Lung Cancer Res

Construction of a lung cancer 3D culture model based on alginate/gelatin micro-beads for drug evaluation. [Abstract]

2024 Oct 31;13(10):2698-2712. PMID: 39507032
Mol Med Rep

Inhibition of Bcl-2 and Bcl-xL overcomes the resistance to the third-generation EGFR tyrosine kinase inhibitor osimertinib in non-small cell lung cancer. [Abstract]

2021 Jan;23(1):48. PMID: 33200796
BMC Cancer

METTL16-dependent miR-146b-5p m6A modification remodeling sensitize NSCLC to osimertinib via activating PI3K/AKT signaling. [Abstract]

2025 Apr 8;25(1):641. PMID: 40200229
Toxicol Appl Pharmacol

Jaceosidin overcomes osimertinib resistance in lung cancer by inducing G2/M cycle arrest through targeting DDB1. [Abstract]

2025 Apr 3:117327. PMID: 40187661
Cancer Res Commun

Constitutive EGFR Activation Induced by PTPRR Downregulation Confers Resistance to KRAS Inhibitors. [Abstract]

2026 Mar 10. PMID: 41808249
Basic Clin Pharmacol Toxicol

GMI, a Fungal Immunomodulatory Protein From Ganoderma microsporum, Induces Different Cytotoxicity in Parental and Osimertinib-Resistant EGFR-Mutated Lung Cancer Cells via Apoptotic and Autophagic Cell Death. [Abstract]

2025 Dec;137(6):e70143. PMID: 41269207
Environ Toxicol

Epithelial growth factor receptor tyrosine kinase inhibitors alleviate house dust mite allergen Der p2-induced IL-6 and IL-8. [Abstract]

2019 Apr;34(4):476-485. PMID: 30623574

Osimertinib purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]

Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

Osimertinib purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]

Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

Osimertinib purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]

Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.
Front Biosci (Landmark Ed)

Integrated Analysis of Single-cell and Bulk-RNA Sequencing Data to Identify Redox-related Genes as Prognostic Biomarkers and Therapeutic Targets of Lung Adenocarcinoma With Osimertinib Resistance. [Abstract]

2025 Sep 25;30(9):40454. PMID: 41074434
RSC Chem Biol

A covalent inhibitor of the YAP-TEAD transcriptional complex identified by high-throughput screening. [Abstract]

2023 Aug 29;4(11):894-905. PMID: 37920398
Genomics

STRIP2 confers acquired resistance to EGFR-TKIs in lung adenocarcinoma by modulating IGF2BP3-dependent Twist1 stability. [Abstract]

2026 May 25;118(4):111262. PMID: 42191053
Mol Pharmacol

Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]

2022 Jun;101(6):381-389. PMID: 35383108
Discov Oncol

Integrative bulk RNA analysis unveils immune evasion mechanisms and predictive biomarkers of osimertinib resistance in non-small cell lung cancer. [Abstract]

2025 Aug 12;16(1):1541. PMID: 40796706
Am J Cancer Res

Luteolin overcomes acquired resistance to osimertinib in non-small cell lung cancer cells by targeting the HGF-MET-Akt pathway. [Abstract]

2023 Sep 15;13(9):4145-4162. PMID: 37818074
Genes (Basel)

The Impact of Bevacizumab and miR200c on EMT and EGFR-TKI Resistance in EGFR-Mutant Lung Cancer Organoids. [Abstract]

2024 Dec 19;15(12):1624. PMID: 39766891
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2024 Apr 15:1237:124100. PMID: 38547701
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
World J Gastrointest Oncol

Interleukin-22 promotes cancer stemness and chemotherapy resistance in colorectal cancer via epidermal growth factor receptor/extracellular signal-regulated kinase pathway. [Abstract]

2025 Aug 15;17(8):108535. PMID: 40837778
J Nat Med

Effects of Ephedra Herb extract on the expression of EGFR-activating mutations and c-Met in non-small-cell lung cancer cell line, H1975, and its combined effects with osimertinib. [Abstract]

2023 Jun;77(3):523-534. PMID: 37043119
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Int J Electrochem Sci

2024 Nov 26.
Eur J Drug Metab Pharmacokinet

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2021 Sep;46(5):625-635. PMID: 34275128
Thorac Cancer

Copy Number Amplification and c-Myc Transcriptional Activation-Mediated RNA-Binding Protein MEX3A Promotes EGFR-TKI Resistance in Non-Small-Cell Lung Cancer. [Abstract]

2026 May;17(9):e70284. PMID: 42080737
Biochem Biophys Res Commun

2026 Feb 12:800:153165. PMID: 41548485
Biochem Biophys Res Commun

Investigating NanoLuc-EGFR engineered cell lines for real-time monitoring of EGFR protein dynamics in live cells. [Abstract]

2024 Sep 19:733:150711. PMID: 39312880
Oncol Lett

Upregulation of long non‑coding RNA LINC00460 in EGFR‑mutant lung cancer indicates a poor prognosis in patients treated with osimertinib. [Abstract]

2023 Jul 20;26(3):380. PMID: 37559586
Drug Metab Pharmacokinet

Characterization of covalent binding of tyrosine kinase inhibitors to plasma proteins. [Abstract]

2020 Oct;35(5):456-465. PMID: 32847720
Genes Genomics

CKAP4 is a potential therapeutic target to overcome resistance to EGFR-TKIs in lung adenocarcinoma. [Abstract]

2025 Mar;47(3):331-340. PMID: 39704929
Cytotechnology

Silencing of LINC01278 promotes sensitivity of non-small cell lung cancer cells to osimertinib by targeting miR-324-3p/ZFX axis. [Abstract]

2025 Feb;77(1):23. PMID: 39711969
Acta Chromatogr

2025 Jan 07.
Anticancer Res

Antitumor Potential of Guttiferone E Combined With Carboplatin Against Osimertinib-resistant H1975 Lung Cancer Through Apoptosis. [Abstract]

2024 Oct;44(10):4175-4188. PMID: 39348999
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An UPLC-MS/MS Method for Determination of Osimertinib in Rat Plasma: Application to Investigating the Effect of Ginsenoside Rg3 on the Pharmacokinetics of Osimertinib. [Abstract]

2020 Dec 28:2020:8814214. PMID: 33456471
Anticancer Res

Brexpiprazole Reduces Survivin and Reverses EGFR Tyrosine Kinase Inhibitor Resistance in Lung and Pancreatic Cancer. [Abstract]

2019 Sep;39(9):4817-4828. PMID: 31519584
Am J Transl Res

EGFR/EGFRvIII partly regulates the tumourigenesis of glioblastoma through the SOX9-GLUT3 axis. [Abstract]

2021 Jun 15;13(6):6055-6065. PMID: 34306344
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Xenobiotica

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bioRxiv

2026 Jun 19.
Res Sq

2026 Apr 28.
bioRxiv

2026 Mar 12.
University of Ioannina

2026.
bioRxiv

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bioRxiv

2025 Oct 17.
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US20250275968A1.
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2025.
State University of New York at Buffalo

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2025 Apr 11.
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bioRxiv

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Research Square Preprint

2024 Dec 02.
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bioRxiv

2024 Feb 12.
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2023 Jun 30.
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Oncotarget

Targeting the Golgi apparatus to overcome acquired resistance of non-small cell lung cancer cells to EGFR tyrosine kinase inhibitors. [Abstract]

2017 Dec 6;9(2):1641-1655. PMID: 29416720
Oncotarget

Discovery and characterization of a novel irreversible EGFR mutants selective and potent kinase inhibitor CHMFL-EGFR-26 with a distinct binding mode. [Abstract]

2017 Mar 14;8(11):18359-18372. PMID: 28407693

Osimertinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372. [Abstract]

In all of the cell lines tested, AZD9291 (Osimertinib) significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

Osimertinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372. [Abstract]

In all of the cell lines tested, AZD9291 (Osimertinib) significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.
Genes Cancer

NSCLC depend upon YAP expression and nuclear localization after acquiring resistance to EGFR inhibitors. [Abstract]

2017 Mar;8(3-4):497-504. PMID: 28680534
Oncotarget

Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. [Abstract]

2016 Oct 25;7(43):69760-69769. PMID: 27626175
Oncotarget

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. [Abstract]

2015 Oct 13;6(31):31313-22. PMID: 26375053

Osimertinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]

Effect of PCI-32765, WZ4002, AZD9291 (Osimertinib) and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (200.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0016 mL

10.0078 mL

20.0156 mL

5 mM

0.4003 mL

2.0016 mL

4.0031 mL

10 mM

0.2002 mL

1.0008 mL

2.0016 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 KB)
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Elemental Analysis Report (2659 KB)
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Références

[1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. [Content Brief]

[2]. Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0016 mL	10.0078 mL	20.0156 mL	50.0390 mL
	5 mM	0.4003 mL	2.0016 mL	4.0031 mL	10.0078 mL
	10 mM	0.2002 mL	1.0008 mL	2.0016 mL	5.0039 mL
	15 mM	0.1334 mL	0.6672 mL	1.3344 mL	3.3359 mL
	20 mM	0.1001 mL	0.5004 mL	1.0008 mL	2.5020 mL
	25 mM	0.0801 mL	0.4003 mL	0.8006 mL	2.0016 mL
	30 mM	0.0667 mL	0.3336 mL	0.6672 mL	1.6680 mL
	40 mM	0.0500 mL	0.2502 mL	0.5004 mL	1.2510 mL
	50 mM	0.0400 mL	0.2002 mL	0.4003 mL	1.0008 mL
	60 mM	0.0334 mL	0.1668 mL	0.3336 mL	0.8340 mL
	80 mM	0.0250 mL	0.1251 mL	0.2502 mL	0.6255 mL
	100 mM	0.0200 mL	0.1001 mL	0.2002 mL	0.5004 mL

Keywords

Osimertinib

202 Cited Publications

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