货号 | 5403/50 |
别名 | 4-[(9-Cyclopentyl-7,7-difluoro-6,7, |
供应商 | Tocris |
生物活性 | Potent PLK1 inhibitor (IC50 values are 0.8, 16.9 and 50.2 nM for PLK1, PLK2 and PLK3 respectively). Exhibits >20-fold selectivity for PLK1 over FAK, MLCK and FES, and has minimal activity against a panel of 282 other kinases. Inhibits proliferation of a range of cancer cell lines in vitro and inhibits tumor growth of multiple human cancer cell xenografts in vivo. Orally bioavailable. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 598.06 |
分子式 | C27H34F3N7 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Nieet al (2013) Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Bioorg.Med.Chem.Lett. 23 3662. PMID: 23664874. Hikichiet al (2012) TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol.Cancer Ther. 11 700. PMID: 22188812. |