IDH889
| CAS号 | 1429179-07-6 | 货号 | BCP32439 |
| 中文名 | IDH889 | ||
| 英文名 | IDH889 | ||
| 中文别名 | |||
| 英文别名 | IDH-889; IDH 889; | ||
| 分子式 | C23H25FN6O2 | 分子量 | 436.48 |
| 生物活性 | IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM. IDH889 demonstrates significantly improved plasma exposure in mice vs IDH662 (AUC 3.6 μM·h, Cmax 1.7 μM at 10 mg/kg; AUC 55.5 μM·h, Cmax 14.2 μM at 100 mg/kg). IDH889 also has excellent permeability and no efflux in the Caco-2 and human MDR1-MDCK cell lines, supporting the hypothesis that potent inhibition of mutant IDH1 function by binding at the allosteric binding site is compatible with brain penetration. | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | IDH | ||
结构式
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