货号 | 4821/50 |
别名 | N-[2-[(1S,4R)-6-[[4-(Cyclobutylamin |
供应商 | Tocris |
生物活性 | ATP-competitive inhibitor of Aurora kinases A and B (IC50 values are 0.8 and 5 nM for recombinant Aurora B and Aurora A, respectively). Inhibits phosphorylation of Aurora B, histone H3 and Aurora A in cultured MDA-MB-231 cells (IC50 values are approximately 20, 50 and 150 nM respectively). Shown to block cytokinesis; inhibits cellular proliferation in several human tumor cell lines, including HCT-116, HL-60, A549 and H125, and in human xenograft mouse models. Orally available. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 474.48 |
分子式 | C23H25F3N6 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 20 mM in ethanol |
参考文献 | Hooket al (2012) An integrated genomic approach to identify predictive biomarkers of response to the Aurora kinase inhibitor PF-03814735. Mol.Cancer Ther. 11 710. PMID: 22222631. Kollareddyet al (2012) Aurora kinase inhibitors: progress towards the clinic. Invest.New Drugs 30 2411. PMID: 22350019. Janiet al (2010) PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol.Cancer Ther. 9 883. PMID: 20354118. |