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| 产品描述 |
| GSK864 is a potent and selective inhibitor of mutant IDH1. GSK864 inhibits IDH1 mutants R132C/R132H/R132G with IC50 values of 9/15/17 nM, respectively, and is moderately selective over wild-type IDH1 and IDH2 mutants/wild-type. Treatment of R132C IDH1 mutant HT-1080 cells for 24 hours with GSK864 results in a dose-dependent reduction of 2-hydroxyglutarate (2-HG), which is not observed with GSK990, a structurally similar compound which is inactive as an IDH1 inhibitor. GSK864 has been shown to be selective in vitro for IDH1 over other classes of proteins (7TMs, ion channels, kinases) and chemoproteomic studies with GSK321, an analog of GSK864, confirm selective binding of IDH1 by this chemical series. GSK864 has a pharmacokinetic profile suitable for in vivo studies. |
| 化学结构 |
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| 化学名称 |
| (S)-1-(4-fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide |
| SMILES Code |
| O=C(C1=NN(CC2=CC=C(F)C=C2)C3=C1CN(C(C4=CC=CN4)=O)C[C@]3(C)C(N)=O)NC5=CC(C)=C(OC)C(C)=C5 |
| 基本信息 |
产品编号:XM477
产品名称:GSK864
别名:GSK864; GSK-864; GSK 864.
CAS#:1816331-66-4
分子式:C30H31FN6O4
精确分子量:558.2391
分子量:558.6144
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| 物化性质 |
外观: 固体粉末
纯度: >98%
运输信息: 非危险化学品，适于常温或冰袋运输。
储存条件: 低温，干燥，避光。
溶解性: 溶于DMSO, 不溶于水
储存期限:3年 -20℃固体储存
2 年 -80℃ 溶液储存 |
该产品只供科研使用，不能给病人提供。
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