| 产品描述： | PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively. |
| 靶点： |
Aurora 1:0.8 nM (IC50);Aurora 2:5 nM (IC50);Flt-1:10 nM (IC50);FAK:22 nM (IC50);TrkA;30 nM (IC50);Met:100 nM (IC50);FGFR1:100 nM (IC50);FAK; VEGFR; FLT; Trkreceptor; AuroraKinase |
| 体内研究： |
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 |
| 参考文献： |
1. Jani JP, et al. PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol Cancer Ther. 2010 Apr;9(4):883-94. 2. Hook KE, et al. An integrated genomic approach to identify predictive biomarkers of response to the aurora kinase inhibitor PF-03814735. Mol Cancer Ther. 2012 Mar;11(3):710-9. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.108 ml |
10.538 ml |
21.076 ml |
| 5 mM |
0.422 ml |
2.108 ml |
4.215 ml |
| 10 mM |
0.211 ml |
1.054 ml |
2.108 ml |
| 50 mM |
0.042 ml |
0.211 ml |
0.422 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京