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- 2025年12月05日
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Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
942487-16-3
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1377.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥569.0 |
| 规格： | 5 mg | 产品价格： | ￥1252.0 |
| 规格： | 10 mg | 产品价格： | ￥2358.0 |
| 规格： | 25 mg | 产品价格： | ￥4250.0 |
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PF-03814735
CAS No. : 942487-16-3
MCE 国际站：PF-03814735
产品活性：PF-03814735是有效，有口服性，ATP 竞争性的，可逆的极光激酶A和B (aurora A/B) 的抑制剂，IC50值分别为0.8和5 nM。
研究领域：Cell Cycle/DNA Damage | Epigenetics | Protein Tyrosine Kinase/RTK
作用靶点：Aurora Kinase | VEGFR
In Vitro: In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. 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.
In Vivo: Once-daily oral administration of PF-03814735 to mice bearing human xenograft tumors produces a reduction in phosphohistone H3 in tumors at doses that are tolerable and that result in significant inhibition of tumor growth. The combination of PF-03814735 and docetaxel in xenograft mouse tumor models shows additive tumor growth inhibition. PF-03814735 is much more effective in NCI-H82 xenografts when administered on a weekly dosing schedule at 80 mg/kg compared with a daily schedule at 15 mg/kg. PF-03814735 delayed growth by 23.5 days on the weekly schedule, which corresponds to 0.9 logs of net cell kill during the course of treatment.
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