| 产品描述: | c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties |
| 靶点: |
c-Kit |
| 体内研究: |
c-Kit-IN-5 (compound 25) (1 mg/kg; i.v.) exhibits CL (0.46 L/h/kg) and Vdss (1.59 L/kg) in rats. c-Kit-IN-5 (10 mg/kg; p.o.) exhibits AUC0-t(9860 ng•h/mL) Cmax(1230 ng/mL), T1/2 (2.6 h), and F (39%) in rats |
| 参考文献: |
1. Hu E, et, al. Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. J Med Chem. 2008 Jun 12;51(11):3065-8 |
| 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 |
2.529 ml |
12.645 ml |
25.29 ml |
| 5 mM |
0.506 ml |
2.529 ml |
5.058 ml |
| 10 mM |
0.253 ml |
1.264 ml |
2.529 ml |
| 50 mM |
0.051 ml |
0.253 ml |
0.506 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。 |