BAY-1436032
  • 化学数据
CAS号 1803274-65-8 货号 BCP18989
中文名 BAY-1436032
英文名 BAY-1436032
中文别名
英文别名 BAY 1436032;BAY1436032;
分子式 C26H30F3N3O3 分子量 489.53
  • 用途
生物活性 BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). BAY 1436032 is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displayed potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. In line with the proposed mode of action, a concentration-dependent lowering of 2-HG was observed in vitro accompanied by differentiation and maturation of mIDH1 tumor cells. Furthermore, BAY 1436032 showed a favourable selectivity profile against wtIDH1/2 and a large panel of off-targets in vitro.
信号通路 Protease/Metabolic Enzyme 
靶 点 IDH 

结构式

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