- 英文名称
- GSK864
- 分子式
- C30H31FN6O4
- 分子量
- 558.6
- 中文别名
- GSK864; 化合物T15442; 化合物GSK864; 异柠檬酸脱氢酶1(IDH1)突变体抑制剂GSK864; (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; (7S)-1-(4-Fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrol-2-ylcarbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide; (7S)-1-[(4-fluorophenyl)methyl]-3-N-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,6-dihydropyrazolo[4,5-c]pyridine-3,7-dicarboxamide; GSK 864; GSK-864; 1H-Pyrazolo[4,3-c]pyridine-3,7-dicarboxamide, 1-[(4-fluorophenyl)methyl]-4,5,6,7-tetrahydro-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrol-2-ylcarbonyl)-, (7S)-; (7S)-1-[(4-fluorophenyl)methyl]-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-1H,4H,5H,6H,7H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide
- 用途
- 作为异柠檬酸脱氢酶1(IDH1)突变体抑制剂，用于生命科学领域；抑制IDH1突变体R132C、R132H和R132G的IC50值分别为8.8、15.2和16.6 nM；体外抑制R132C IDH1突变体HT1080细胞中2-HG产生，EC50为320 nM；体内腹腔注射后在小鼠外周血中维持有效浓度达24小时，可增加早期分化标记物表达的细胞数量。
