IDH-889
产品编号: DC10830
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应用领域
IDH889 是一种可口服利用的，脑渗透性的，变构和突变特异性的异柠檬酸脱氢酶 (IDH1) 抑制剂。IDH889 对 IDH1 R132* 突变型具有高效选择性，对 IDH1R132H、IDH1R132C 和 IDH1wt 作用的 IC50 值分别为 0.02 μM, 0.072 μM 和 1.38 μM。IDH889 具有高效的细胞内 2-HG 水平抑制作用，其 IC50 值为 0.014 μM。
| Cas No.: |
1429179-07-6 |
| 名称: |
(S)-3-(2-(((S)-1-(5-(4-fluoro-3-methylphenyl)pyrimidin-2-yl)ethyl)amino)pyrimidin-4-yl)-4-isopropyloxazolidin-2-one |
| 别名: |
IDH889,IDH-889,IDH 889 |
| SMILES: |
CC1=C(F)C=CC(C2=CN=C([C@@H](NC3=NC(N4[C@@H](C(C)C)COC4=O)=CC=N3)C)N=C2)=C1 |
| 分子式: |
C23H25FN6O2 |
| 分子量: |
436.2 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| References: |
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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MSDS
| TITLE |
DOWNLOAD |
| MSDS_572_DC10830_1429179-07-6 |
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COA
| LOT NO. |
DOWNLOAD |
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