CH7233163 | mutant EGFR inhibitor | Probechem Biochemicals

Chemical Structure : CH7233163

CAS No.: 2923365-71-1

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CH7233163 (CH 7233163)

货号: PC-38170Not For Human Use, Lab Use Only.

CH7233163 is a novel potent, selective mutant EGFR-Del19/T790M/C797S inhibitor with IC50 of 0.28 nM in biochemical assays.

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生物&药学活性

CH7233163 is a novel potent, selective mutant EGFR-Del19/T790M/C797S inhibitor with IC50 of 0.28 nM in biochemical assays.
EAI-045, an allosteric EGFR inhibitor, didn't show inhibitory activity in this assay (IC50>1 uM).
CH7233163 potently inhibited the proliferation of Del19/T790M/C797S_NIH3T3 cells with IC50 of 20 nM, potently and dose dependently blocked the EGFR phosphorylation.
CH7233163 more selectively inhibits various types of EGFR mutants (e.g., L858R/T790M/C797S, L858R/T790M, Del19/T790M, Del19, and L858R) over wild type.
CH7233163 potently inhibited not only EGFR-Del19/T790M/C797S but also various EGFR mutations, including L858R/T790M/C797S triple mutations, double mutations and single-activating-mutations.

物理化学性质&存储条件

分子量	669.728
分子式	C31H34F3N9O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(2-(1-(cyclopropylsulfonyl)-1H-pyrazol-4-yl)pyrimidin-4-yl)-5-isopropyl-7-(4-methylpiperazin-1-yl)-9-(2,2,2-trifluoroethoxy)-5H-pyrido[4,3-b]indol-3-amine

参考文献

1. Kenji Kashima, et al. Mol Cancer Ther. 2020 Nov;19(11):2288-2297.

CH7233163 (CH 7233163)

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物理化学性质&存储条件

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CH7233163 (CH 7233163)

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