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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-BBT-176
BBT-176

Chemical Structure : BBT-176

CAS No.: 2254805-55-3

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BBT-176 (BBT176)

货号: PC-23647Not For Human Use, Lab Use Only.

BBT-176 is a potent, mutant-selective fourth-generation inhibitor of EGFR C797S mutations with IC50 of 4.36, 1.79, and 5.35 nM for EGFR 19Del/C797S, EGFR 19Del/T790M/C797S, and EGFR L858R/C797S, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BBT-176 is a potent, mutant-selective fourth-generation inhibitor of EGFR C797S mutations with IC50 of 4.36, 1.79, and 5.35 nM for EGFR 19Del/C797S, EGFR 19Del/T790M/C797S, and EGFR L858R/C797S, respectively.
BBT-176 selectively and noncovalently inhibits triple-mutant EGFR 19Del/T790M/C797S and L858R/T790M/C797S at nanomolar concentrations.
BBT-176 has IC50 of 42, 49, 183, and 202 nM against Ba/F3 cells expressing EGFR 19Del/C797S, EGFR 19Del/T790M/C797S, EGFR L858R/C797S, and EGFR L858R/T790M/C797S, respectively.
BBT-176 strongly inhibited the tumor growth, and in some conditions induced tumor regression in mouse models.

物理化学性质&存储条件

分子量 587.14
分子式 C27H35ClN8O3S
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-((5-chloro-2-((2-methoxy-4-(4-(piperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)methanesulfonamide

参考文献

1. Lim SM, et al. Clin Cancer Res. 2023 Aug 15;29(16):3004-3016.

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