- 英文名称
- N-(6,6-Dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-methylbutanamide
- 分子式
- C19H31N5O2
- 分子量
- 361.48
- 中文别名
- 3-甲基-N-[1,4,5,6-四氢-6,6-二甲基-5-[(1-甲基-4-哌啶基)甲酰基]吡咯并[3,4-C]吡唑-3-基]丁酰胺; PHA-793887; PHA 793887; PHA793887; PHA-793887; N-[6,6-dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4-dihydropyrrolo[3,4-c]pyrazol-3-yl]-3-methylbutanamide; N-{6,6-Dimethyl-5-[(1-methyl-4-piperidinyl)carbonyl]-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl}-3-methylbutanamide; N-(6,6-Dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4,5,6-tetrahydropyrrolo(3,4-C)pyrazol-3-yl)-3-methylbutanamide; 3-Methyl-N-[1,4,5,6-tetrahydro-6,6-dimethyl-5-[(1-methyl-4-piperidinyl)carbonyl]pyrrolo[3,4-c]pyrazol-3-yl]butanamide; N-(6,6-dimethyl-5-(1-methylpiperidine-4-carbonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-methylbutanamide; PHA793887
- 用途
- 化学合成；作为新型有效的CDK2、CDK5和CDK7抑制剂，IC50分别为8 nM、5 nM和10 nM，作用于CDK2、5、7比作用于CDK1、4、9选择性高6倍以上；抑制多种肿瘤细胞系增殖，IC50为88nM–3.4 μM；对白血病细胞系有细胞毒性，IC50为0.3–7 μM，对正常细胞无毒性；诱导细胞周期停滞，抑制Rb和核磷蛋白磷酸化，调节cyclin E和cdc6表达，诱导凋亡；在人类卵巢癌、结肠癌、胰脏癌及白血病移植瘤模型中具有高效性。
