| 货号 | 18388-50mg |
| 描述 | PHA-793887 is a pyrrolo[3,4-c]pyrazole that inhibits cyclin-dependent kinases Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H with IC50 values of 8, 8, 5, and 10 nM, respectively.1 It is more than 6-fold selective for these kinases over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T, and GSK3β (IC50s = 60, 62, 138, and 79 nM, respectively).1 PHA-793887 is cytotoxic to human ovarian A2780, colon HCT116, pancreatic BX-PC3, and leukemic K562, KU812, KCL22, and TOM1 cells both in vitro and in xenograft models.1,2 This compound has been examined in patients with solid tumors in phase 1 clinical trials.3 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Brasca, M.G.,Albanese, C.,Alzani, R., et al. Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioor.Med.Chem. 18, 1844-1853 (2010). 2.Alzani, R.,Pedrini, O.,Albanese, C., et al. Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models. Experimental Hematology 38, 259-269 (2010). 3.Massard, C.,Soria, J.C.,Anthoney, D.A., et al. A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexprected hepatotoxicity in patients with solid tumors. Cell Cycle 10(6), 963-970 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 361.5 |
| 分子式 | C19H31N5O2 |
| CAS号 | 718630-59-2 |
| 稳定性 | ≥ 2 years |
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