产品描述: | CYC-116 is a potent aurora A and aurora B inhibitor with Kis of 8 and 9 nM, respectively. |
靶点: |
Aurora A:8 nM (Ki);Aurora B:9.2 nM (Ki) |
体内研究: |
Oral administration of CYC-116 at dose levels of 75 and 100 mg/kg q.d. causes tumor growth delays of 2.3 and 5.8 days, which translates into specific growth delays of 0.32 and 0.81, respectively. The mean relative tumor volumes of mice receiving CYC-116 at both dose levels are less than those of vehicle-treated mice for the duration of the study period. At 100 mg/kg po q.d., the reduction in growth is statistically significant on days 6 and 9 |
参考文献: |
1. Wang S, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78. |
溶解性: |
DMSO : 15 mg/mL (40.71 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.714 ml |
13.57 ml |
27.14 ml |
5 mM |
0.543 ml |
2.714 ml |
5.428 ml |
10 mM |
0.271 ml |
1.357 ml |
2.714 ml |
50 mM |
0.054 ml |
0.271 ml |
0.543 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。 |