| 产品描述： | TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts |
| 靶点： |
PLK1:0.8 nM (IC50);PLK2:16.9 nM (IC50);PLK3:50.2 nM (IC50);FAK/PTK2:19.6 nM (IC50);MLCK/MYLK:25.6 nM (IC50);FES/FPS:58.2 nM (IC50);PLK |
| 体内研究： |
TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. In animal models, TAK-960 (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts |
| 参考文献： |
1. Hikichi Y, et al. 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. 2012 Mar;11(3):700-9. 2. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666. |
| 溶解性： |
DMSO : 16.67 mg/mL (29.68 mM; ultrasonic and warming and heat to 60°C) |
| 保存条件： |
RT |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.781 ml |
8.903 ml |
17.806 ml |
| 5 mM |
0.356 ml |
1.781 ml |
3.561 ml |
| 10 mM |
0.178 ml |
0.89 ml |
1.781 ml |
| 50 mM |
0.036 ml |
0.178 ml |
0.356 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