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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; | ||
SMILES | CC1=C(C=CC(=C1)C2=CN=C(N=C2)C(C)NC3=NC=CC(=N3)N4C(COC4=O)C(C)C)F | ||
化学名称 | |||
分子式 | C23H25FN6O2 | 分子量 | 436.48 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | 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. |
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