DS06652923 | EGFR C797S inhibitor | Probechem Biochemicals

Chemical Structure : DS06652923

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DS06652923 (DS 06652923)

货号: PC-22888Not For Human Use, Lab Use Only.

DS06652923 is a potent, and orally available EGFR-triple-mutant inhibitor with IC50 of 2.0 nM, 0.89 nM and 6.0 nM for del19/T790M/C797S, L858R/T790M/C797S and WT EGFR resceptively.

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生物&药学活性

DS06652923 is a potent, and orally available EGFR-triple-mutant inhibitor with IC50 of 2.0 nM, 0.89 nM and 6.0 nM for del19/T790M/C797S, L858R/T790M/C797S and WT EGFR resceptively.
DS06652923 shows potent and selective growth inhibition against Ba/F3 EGFR del19/T90M/C797S cells with GI50 of 9.4 nM, with weak activity against Wildtype Ba/F3 (GI50=760 nM).
DS06652923 inhibits only 14 of the 161 kinases (including 6 mutated EGFR) by more than 50 % at 200 nM.
DS06652923 (12.5 mg/kg (bid), 25 mg/kg (qd), 25 mg/kg (bid), and 100 mg/kg (qd), p.o.) dose-dependent antitumor activity with TGI of 88 %, 111 %, 119 %, and 127 %, respectively, in Balb/c nude mice bearing engineered Ba/F3 (EGFR del19/T790M/C797S) tumors.

物理化学性质&存储条件

分子量	629.69
分子式	C28H33F2N9O4S
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	2-[1-(Cyclopropylsulfonyl)-1H-pyrazol-4-yl]-N-{5-[3-(difluoromethoxy)-1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl]-4-(propan-2-yloxy)pyridin-2-yl}pyrimidin-4-amine

参考文献

1. Kageji H, et al. Bioorg Med Chem. 2024 Jul 30;111:117862.

DS06652923 (DS 06652923)

生物&药学活性

物理化学性质&存储条件

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DS06652923 (DS 06652923)

生物&药学活性

物理化学性质&存储条件

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