EGFR-IN-97

Cat. No.: HY-157432: Data Sheet Handling Instructions
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EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR^{L858R/T790M/C797S} and Ba/F3-EGFR^{Del19/T790M/C797S} cells, with IC₅₀ values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR^{L858R/T790M/C797S} cells at the concentration of 0.8 μM.

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EGFR-IN-97 Chemical Structure

CAS No. : 3020681-05-1

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	5.14 μM Compound: 6q	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]
BEAS-2B	IC₅₀	5.12 μM Compound: 6q	Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell growth Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell growth	[PMID: 38142512]
BaF3	IC₅₀	0.41 μM Compound: 6q	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	0.41 μM Compound: 6q	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	0.42 μM Compound: 6q	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]
NCI-H1975	IC₅₀	0.82 μM Compound: 6q	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	2.95 μM Compound: 6q	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]

In Vitro

EGFR-IN-97 (compound 6q) shows excellent activity against mutant NSCLC cell line NCI-H1975-EGFR^{L858R/T790M/C797S} cells, with IC₅₀ value of 0.82 μM, which was superior to that of osimertinib (HY-15772) (IC₅₀ = 2.94 μM), JBJ-04-125-02 (HY-135805) (IC₅₀ = 3.66 μM), and coadministration of JBJ-04-125-02 and osimertinib (IC₅₀ = 1.25 μM)^[1].

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

Molecular Weight

624.73

Formula

C₃₇H₃₆N₈O₂

CAS No.

3020681-05-1

SMILES

NC1=NC=CC(NC(C=C2)=CC=C2NC([C@@H](C3=CC=CC=C3)N4CC5=CC(C6=CC=C(N7CCN(CC7)C)C=C6)=CC=C5C4=O)=O)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hu L, et al. Identification of novel aminopyrimidine derivatives for the treatment of mutant NSCLC. Eur J Med Chem. 2023 Dec 20;265:116074. [Content Brief]

EGFR-IN-97 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR-IN-973020681-05-1EGFRApoptosisEpidermal growth factor receptorErbB-1HER1NCI-H1975Ba/F3NSCLCInhibitorinhibitorinhibit

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