PF-03814735
| CAS号 | 942487-16-3 | 货号 | BCP02851 |
| 中文名 | PF-03814735 | ||
| 英文名 | PF-03814735 | ||
| 中文别名 | |||
| 英文别名 | PF 03814735;PF03814735; | ||
| 分子式 | C23H25F3N6O2 | 分子量 | 474.48 |
| 生物活性 | In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1 (Thr 232, a sensitive marker of Aurora1 activity, with IC50 ~ 20 nM), phosphohistone H3 (with IC50 ~ 50 nM), and phospho-Aurora2 (with IC50 ~150 nM). PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. A recent research indicates small cell lung cancer (SCLC) and, to a lesser extent, colon cancer lines are very sensitive to PF-03814735. The status of the Myc gene family and retinoblastoma pathway members significantly correlates with the efficacy of PF-03814735. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | Aurora VEGFR FAK | ||
结构式
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