- 英文名称
- AZD4573
- 分子式
- C22H28ClN5O2
- 分子量
- 429.94
- 中文别名
- AZD-4573; 化合物AZD4573; (1S,3R)-3-乙酰氨基-N-(5-氯-4-(5,5-二甲基-5,6-二氢-4H-吡咯并[1,2-B]吡唑-3-基)吡啶-2-基)环己烷甲酰胺; (1S,3R)-3-乙酰氨基-N-[5-氯-4-(5,5-二甲基-5,6-二氢-4H-吡咯并[1,2-B]吡唑-3-基)-2-吡啶基]环己烷甲酰胺; AZD 4573; (1S,3R)-3-acetamido-N-[5-chloro-4-(5,5-dimethyl-4,6-dihydropyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl]cyclohexane-1-carboxamide; (1S,3R)-N-(5-chloro-4-{5,5-dimethyl-4H,5H,6H-pyrrolo[1,2-b]pyrazol-3-yl}pyridin-2-yl)-3-acetamidocyclohexane-1-carboxamide; Cyclohexanecarboxamide, 3-(acetylamino)-N-[5-chloro-4-(5,6-dihydro-5,5-dimethyl-4H-pyrrolo[1,2-b]pyrazol-3-yl)-2-pyridinyl]-, (1S,3R)-; (1S,3R)-3-acetamido-N-(5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl)cyclohexane-1-carboxamide; (1S,3R)-3-Acetamido-N-(5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl)cyclohexanecarboxamide
- 用途
- 作为有效的CDK9抑制剂（IC50<0.004 μM），具有高选择性；在细胞中短期处理可减少胞内pSer2-RNAPII，激活caspase3和细胞凋亡，在血液癌细胞系中诱导caspase快速激活（6h）并丧失生存活力（24h），对实体瘤影响甚微；在动物模型中半衰期短（大鼠、狗和猴体内<1h），静脉注射溶解性良好。
