Cat. No.: HY-12857

Brigatinib

(Synonyms: AP-26113)

31 Cited Publications

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Based on 31 publication(s) in Google Scholar

Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC.

For research use only. We do not sell to patients.

Purity: 99.98%
CAS No.: 1197953-54-0
Formula: C₂₉H₃₉ClN₇O₂P
Molecular Weight:584.09

Storage:

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

Brigatinib Chemical Structure

CAS No.: 1197953-54-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (31)
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- In Vivo
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Biological Activity

Description

Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC^[1].

IC₅₀ & Target

IC50: 0.6 nM (ALK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	EC₅₀	936 nM Compound: 14	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	0.5 μM Compound: AP26113	Antiproliferative activity against human A-431 cells by MTT assay Antiproliferative activity against human A-431 cells by MTT assay	[PMID: 37336419]
A-431	IC₅₀	0.51 μM Compound: Brigatinib	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	1.359 nM Compound: 6	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	539.6 nM Compound: 6	Antiproliferative activity against human A-431 cells harboring wild type EGFR incubated for 72 hrs by SRB assay Antiproliferative activity against human A-431 cells harboring wild type EGFR incubated for 72 hrs by SRB assay	[PMID: 37783102]
A-431	IC₅₀	708.7 nM Compound: Brigatinib	Cytotoxicity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37269687]
A-431	IC₅₀	709 nM Compound: Brigatinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
A549	IC₅₀	0.371 μM Compound: Brigatinib	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	910.6 nM Compound: Brigatinib	Antiproliferative activity against human A549 cells harboring wildtype EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells harboring wildtype EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 38676656]
BaF3	EC₅₀	295 nM Compound: 14	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	IC₅₀	<100 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
BaF3	IC₅₀	0.065 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/Del19/T790M mutant Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/Del19/T790M mutant	[PMID: 38908104]
BaF3	IC₅₀	0.071 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/L858R/T790M mutant Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/L858R/T790M mutant	[PMID: 38908104]
BaF3	IC₅₀	0.155 μM Compound: 9	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	0.17 μM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	0.26 μM Compound: 5	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	0.286 μM Compound: 9	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	0.42 μM Compound: 5	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	0.42 μM Compound: Brigatinib	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	0.492 nM Compound: 6	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	IC₅₀	0.56 μM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	0.61 μM Compound: 6	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	0.63 μM Compound: Brigatinib	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	1 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	1.91 μM Compound: 6	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	1.959 μM Compound: Brigatinib	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	IC₅₀	10 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	10 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	12 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	19 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	20 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	30 nM Compound: 1; AP26113	Synergistic antiproliferative activity against mouse BaF3 cells harbouring Del19/T790M/C797S triple mutant in presence of antibody cetuximab Synergistic antiproliferative activity against mouse BaF3 cells harbouring Del19/T790M/C797S triple mutant in presence of antibody cetuximab	[PMID: 34323489]
BaF3	IC₅₀	3214 nM Compound: AP26113	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3 Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3	[PMID: 27780853]
BaF3	IC₅₀	3214 nM Compound: AP26113	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 27780853]
BaF3	IC₅₀	35 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	35 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	36 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	39.9 nM Compound: 15	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	39.9 nM Compound: 7	Cytotoxicity against mouse BaF3 cells expressing EGFR-Del19/L858R mutant assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against mouse BaF3 cells expressing EGFR-Del19/L858R mutant assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 36417820]
BaF3	IC₅₀	4.191 μM Compound: 9	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	433 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
BaF3	IC₅₀	47 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	48 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	542.5 nM Compound: Brigatinib	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant	[PMID: 38331226]
BaF3	IC₅₀	55.5 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay	[PMID: 35413415]
BaF3	IC₅₀	67.2 nM Compound: 15	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	67.2 nM Compound: 7	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 36417820]
BaF3	IC₅₀	67.2 nM Compound: Brigatinib	Inhibition of cell viability in mouse BaF3 cells harboring EGFR C797S/T790M/del19 mutant incubated for 72 hrs by Cell Titer Glo assay Inhibition of cell viability in mouse BaF3 cells harboring EGFR C797S/T790M/del19 mutant incubated for 72 hrs by Cell Titer Glo assay	[PMID: 38908104]
BaF3	IC₅₀	7.31 μM Compound: Brigatinib	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	8.49 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
BaF3	IC₅₀	93 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	98 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
DEL	GI₅₀	31 nM Compound: AP26113	Growth inhibition of human DEL cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of human DEL cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
HaCaT	IC₅₀	5.021 μM Compound: Brigatinib	Cytotoxicity against human HaCaT cells Cytotoxicity against human HaCaT cells	[PMID: 38908104]
HCC827	IC₅₀	0.003 μM Compound: Brigatinib	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	0.013 μM Compound: AP26113	Antiproliferative activity against human HCC827 cells by MTT assay Antiproliferative activity against human HCC827 cells by MTT assay	[PMID: 37336419]
HCC827	IC₅₀	282.4 nM Compound: 6	Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant incubated for 72 hrs by SRB assay Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant incubated for 72 hrs by SRB assay	[PMID: 37783102]
HEK-293T	IC₅₀	850 nM Compound: Brigatinib	Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs	[PMID: 34138566]
HK-2	IC₅₀	2.134 μM Compound: Brigatinib	Cytotoxicity against human HK-2 cells Cytotoxicity against human HK-2 cells	[PMID: 38908104]
HUVEC	IC₅₀	2.171 μM Compound: Brigatinib	Cytotoxicity against human HUVEC cells Cytotoxicity against human HUVEC cells	[PMID: 38908104]
HUVEC	IC₅₀	2.399 μM Compound: Brigatinib	Cytotoxicity against VEGF-stimulated human HUVEC cells Cytotoxicity against VEGF-stimulated human HUVEC cells	[PMID: 38908104]
KARPAS-299	GI₅₀	10 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
KARPAS-299	GI₅₀	10 nM Compound: AP26113	Growth inhibition of human Karpas-299 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of human Karpas-299 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
KARPAS-299	IC₅₀	29 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
L02	IC₅₀	1.399 μM Compound: Brigatinib	Cytotoxicity against human L02 cells Cytotoxicity against human L02 cells	[PMID: 38908104]
LoVo	IC₅₀	2.03 μM Compound: 6	Inhibition of wild type EFGR expressed in human LoVo cell line assessed as inhibition of EGF-stimulated EGFR phosphorylation potency measured after 2 hrs by HRTF assay Inhibition of wild type EFGR expressed in human LoVo cell line assessed as inhibition of EGF-stimulated EGFR phosphorylation potency measured after 2 hrs by HRTF assay	[PMID: 34491761]
NCI-H1299	IC₅₀	1.049 μM Compound: 9	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-H1975	IC₅₀	0.32 μM Compound: Brigatinib	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	0.424 μM Compound: Brigatinib	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	0.62 μM Compound: Brigatinib	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	0.64 μM Compound: Brigatinib	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	0.83 μM Compound: AP26113	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	1.09 μM Compound: 5	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	IC₅₀	1134 nM Compound: 6	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by SRB assay	[PMID: 37783102]
NCI-H1975	IC₅₀	379.9 nM Compound: 6	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by SRB assay	[PMID: 37783102]
NCI-H1975	IC₅₀	444.4 nM Compound: Brigatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 38676656]
NCI-H2228	GI₅₀	10 nM Compound: AP26113	Growth inhibition of human NCI-H2228 cells harboring EML4-ALK v3a/3b incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of human NCI-H2228 cells harboring EML4-ALK v3a/3b incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
NCI-H2228	IC₅₀	31.2 nM Compound: Brigatinib	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
NCI-H2228	IC₅₀	58.2 nM Compound: Brigatinib	Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 32179332]
NCI-H23	GI₅₀	1337 nM Compound: AP26113	Growth inhibition of ALK-negative human NCI-H23 cells incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of ALK-negative human NCI-H23 cells incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
NCI-H3122	GI₅₀	4 nM Compound: AP26113	Growth inhibition of human NCI-H3122 cells harboring EML4-ALK v1 incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of human NCI-H3122 cells harboring EML4-ALK v1 incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
NCI-H69	IC₅₀	2.6 μM Compound: Brigatinib	Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell proliferation Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell proliferation	[PMID: 32179332]
NCI-H838	GI₅₀	503 nM Compound: AP26113	Growth inhibition of ALK-negative human NCI-H838 cells incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of ALK-negative human NCI-H838 cells incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
PC-9	IC₅₀	0.087 μM Compound: Brigatinib	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	0.39 μM Compound: Brigatinib	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	0.829 μM Compound: 9	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	1.11 μM Compound: 9	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	1.454 nM Compound: 6	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	109.8 nM Compound: Brigatinib	Antiproliferative activity against human PC-9 cells harboring EGFR exon 19 deletion mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells harboring EGFR exon 19 deletion mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 38676656]
PC-9	IC₅₀	132.8 nM Compound: Chemical Probe: Brigatinib	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	243.8 nM Compound: Chemical Probe: Brigatinib	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	599.2 nM Compound: Brigatinib	Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay	[PMID: 35413415]
PC-9	IC₅₀	599.2 nM Compound: Chemical Probe: Brigatinib	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	838.4 nM Compound: 6	Antiproliferative activity against human PC-9 cells harboring EGFR Del19/T790M/C797S mutant incubated for 72 hrs by SRB assay Antiproliferative activity against human PC-9 cells harboring EGFR Del19/T790M/C797S mutant incubated for 72 hrs by SRB assay	[PMID: 37783102]
Sf9	IC₅₀	0.001 μM Compound: Brigatinib	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	0.001 μM Compound: Brigatinib	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	0.13 μM Compound: Brigatinib	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]
Sf9	IC₅₀	3 nM Compound: 3	Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	[PMID: 31298540]
SR	IC₅₀	1.9 nM Compound: Brigatinib	Antiproliferative activity against ALK positive human SR cells Antiproliferative activity against ALK positive human SR cells	[PMID: 33751979]
SR	IC₅₀	2.7 nM Compound: Brigatinib	Antiproliferative activity against human SR cells assessed as reduction in cell growth Antiproliferative activity against human SR cells assessed as reduction in cell growth	[PMID: 32179332]
SR	IC₅₀	3.3 nM Compound: Brigatinib	Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 34138566]
SU-DHL-1	GI₅₀	9 nM Compound: AP26113	Growth inhibition of human SU-DHL-1 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of human SU-DHL-1 cells harboring NPM-ALK incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
U-937	GI₅₀	2387 nM Compound: AP26113	Growth inhibition of ALK-negative human U-937 cells incubated for 72 hrs by CyQuant cell proliferation assay Growth inhibition of ALK-negative human U-937 cells incubated for 72 hrs by CyQuant cell proliferation assay	[PMID: 27780853]
U-937	IC₅₀	3194 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]

In Vitro

Brigatinib potently inhibits the in vitro kinase activity of ALK (IC₅₀, 0.6 nM) and all five mutant variants tested, including G1202R (IC₅₀, 0.6-6.6 nM).
Brigatinib demonstrates a high degree of selectivity, only inhibiting 11 additional native or mutant kinases with IC₅₀ <10 nM. These include ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR (L858R; IC₅₀, 1.5-2.1 nM).
Brigatinib exhibits more modest activity against EGFR with a T790M resistance mutation (L858R/T790M), native EGFR, IGF1R, and INSR (IC₅₀, 29-160 nM) and does not inhibit MET (IC₅₀ >1000 nM).
In cellular assays, brigatinib inhibits ALK and ROS1 with IC₅₀s of 14 and 18 nM, respectively.
Brigatinib inhibits FLT3 and IGF-1R with about 11-fold lower potency (IC₅₀, 148-158 nM) and inhibits mutant variants of FLT3 and EGFR with 15- to 35-fold lower potency (IC₅₀, 211-489 nM).
Brigatinib inhibits cell growth with GI₅₀ values ranging from 503 to 2,387 nM in three ALK-negative ALCL and NSCLC cell lines^[1].
Brigatinib inhibits ALK activity and abrogates proliferation of ALK addicted neuroblastoma cell lines, with IC₅₀ of 75.27 ± 8.89 nM.
Brigatinib inhibits both the ALK-I1171N and the ALK-G1269A mutant receptors at 10 and 4 nM levels, respectively^[3].

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

In Vivo

Brigatinib (10, 25, or 50 mg/kg once daily, p.o.) leads to a dose-dependent inhibition of tumor growth in ALK⁺ Karpas-299 (ALCL) and H2228 (NSCLC) xenograft mouse models. Brigatinib markedly enhances survival of mice bearing ALK⁺ brain tumors compared with PF-02341066^[1].
Brigatinib (10, 25, 50 mg/kg, p.o.) results in dose-dependent antitumor activity, with tumor regressions in a mouse model of NSCLC^[2].

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

Clinical Trial

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

Chemical Information

CAS No. 1197953-54-0
Appearance Solid
Molecular Weight 584.09
Formula C₂₉H₃₉ClN₇O₂P
Color Light yellow to green yellow
SMILES

CN1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C(OC)=C3)CC2)CC1
Synonyms

AP-26113
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (31)

All Cell Proliferation/Viability AssayWBIF

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Journal Impact Factor

Nat Biotechnol

Comprehensive profiling of clinically approved kinase inhibitors reveals mutation-specific inhibitors and opportunities for drug repurposing. [Abstract]

2026 Apr 20. PMID: 42010121
Cancer Discov

NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]

2024 Sep 13:OF1-OF20. PMID: 39269178
Cancer Discov

Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer. [Abstract]

2018 Jun;8(6):714-729. PMID: 29650534
Nat Cancer

Analysis of lorlatinib analogs reveals a roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer. [Abstract]

2022 Jun;3(6):710-722. PMID: 35726063
Nat Commun

Linker-free PROTACs efficiently induce the degradation of oncoproteins. [Abstract]

2025 May 23;16(1):4794. PMID: 40410168

Brigatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 23;16(1):4794. [Abstract]

Assessment of cell viability in BaF3-EML4-ALK cells treated with 1 μM Brigatinib (0.5-24 h) at the indicated time points was performed using the CCK8 assay.
Nat Commun

Targeting NRAS via miR-1304-5p or farnesyltransferase inhibition confers sensitivity to ALK inhibitors in ALK-mutant neuroblastoma. [Abstract]

2024 Apr 23;15(1):3422. PMID: 38653965

Brigatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Apr 23;15(1):3422. [Abstract]

SH-SY5Y cell viability and ALK TKI ED₅₀s, 5 days post transfection of the indicated miRNA inhibitors followed by 72 h exposure to either Brigatinib.
Acta Pharm Sin B

2026 Mar 2.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Theranostics

Repurposing Brigatinib for the Treatment of Colorectal Cancer Based on Inhibition of ER-phagy. [Abstract]

2019 Jul 9;9(17):4878-4892. PMID: 31410188

Brigatinib purchased from MedChemExpress. Usage Cited in: Theranostics. 2019 Jul 9;9(17):4878-4892. [Abstract]

LDH release assay of DLD-1 and HCT116 cells treated with the indicated concentrations of Brigatinib for 24 hours.

Brigatinib purchased from MedChemExpress. Usage Cited in: Theranostics. 2019 Jul 9;9(17):4878-4892. [Abstract]

Immunoblotting of total and cleaved PARP or caspase 3 in CRC cells treated with the indicated concentrations of Brigatinib (0.05-2 μM) for 24 hours.

Brigatinib purchased from MedChemExpress. Usage Cited in: Theranostics. 2019 Jul 9;9(17):4878-4892. [Abstract]

Immunofluorescence analysis of ORP8 in CRC cells treated with 1 μM Brigatinib for 12 hours. Scale bar, 10 μm. The results showed that Brigatinib induced the upregulation of ORP8.
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
Pharmacol Res

P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability. [Abstract]

2018 Nov:137:47-55. PMID: 30253203
Neoplasia

ALK inhibitors downregulate the expression of death receptor 4 in ALK-mutant lung cancer cells via facilitating Fra-1 and c-Jun degradation and subsequent AP-1 suppression. [Abstract]

2023 Aug:42:100908. PMID: 37192591
J Med Chem

Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations. [Abstract]

2024 Oct 24;67(20):18098-18123. PMID: 39361251
J Med Chem

Distinct Amino Acid-Based PROTACs Target Oncogenic Kinases for Degradation in Non-Small Cell Lung Cancer (NSCLC). [Abstract]

2024 Aug 22;67(16):13666-13680. PMID: 39114932
Pharmaceutics

Interaction of ALK Inhibitors with Polyspecific Organic Cation Transporters and the Impact of Substrate-Dependent Inhibition on the Prediction of Drug-Drug Interactions. [Abstract]

2023 Sep 13;15(9):2312. PMID: 37765282
Spectrochim Acta A Mol Biomol Spectrosc

Novel spectrofluorimetric determination of brigatinib in bulk powder and human urine samples via ion-pair complex formation using eosin Y. [Abstract]

2021 Mar 15:249:119210. PMID: 33234480
RSC Adv

2018 8:1182-1190.
Cancers (Basel)

BRG1 and NPM-ALK Are Co-Regulated in Anaplastic Large-Cell Lymphoma; BRG1 Is a Potential Therapeutic Target in ALCL. [Abstract]

2021 Dec 29;14(1):151. PMID: 35008316
iScience

Metabolic stratification of human breast tumors reveal subtypes of clinical and therapeutic relevance. [Abstract]

2023 Sep 26;26(10):108059. PMID: 37854701
Transl Oncol

Anti-epidermal growth factor vaccine antibodies increase the antitumor activity of kinase inhibitors in ALK and RET rearranged lung cancer cells. [Abstract]

2021 Jan;14(1):100887. PMID: 33129112
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
ChemMedChem

Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2). [Abstract]

2017 Nov 22;12(22):1857-1865. PMID: 28952188
Mol Immunol

ALK-JNK signaling promotes NLRP3 inflammasome activation and pyroptosis via NEK7 during Streptococcus pneumoniae infection. [Abstract]

2023 May:157:78-90. PMID: 37001294
Clin Chim Acta

Investigation of metabolic stability of the novel ALK inhibitor brigatinib by liquid chromatography tandem mass spectrometry. [Abstract]

2018 May:480:180-185. PMID: 29458050
Fundam Clin Pharmacol

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

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Biomed Chromatogr

Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]

2024 Oct;38(10):e5986. PMID: 39136165
Biomed Chromatogr

Development and validation of an HPLC-MS/MS method to simultaneously quantify brigatinib, lorlatinib, pralsetinib and selpercatinib in human K2-EDTA plasma. [Abstract]

2023 Jun;37(6):e5628. PMID: 36941218
Biol Pharm Bull

An Indirect Competitive Enzyme-Linked Immunosorbent Assay for the Determination of Brigatinib and Gilteritinib Using a Specific Polyclonal Antibody. [Abstract]

2022;45(7):904-909. PMID: 35786598
bioRxiv

2026 Mar 28.
Maastricht University

2023 Jun 1.

Solvent & Solubility

In Vitro:

Ethanol : 5 mg/mL (8.56 mM; ultrasonic and warming and heat to 60°C)

DMSO : 2 mg/mL (3.42 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

1.7121 mL

8.5603 mL

17.1206 mL

5 mM

0.3424 mL

1.7121 mL

3.4241 mL

10 mM

---

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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% EtOH 90% Corn Oil

Solubility: ≥ 1 mg/mL (1.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 EtOH stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

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