| 产品描述: | VEGFR2 选择性抑制剂;VEGFR2 Selective Inhibitors;;InformationCS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selectiveVEGFR-2inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such asRET (c-RET)andKit (c-Kit)with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.TargetsVEGFR2 (Cell-free assay); RET (Cell-free assay); Kit (Cell-free assay) 40 nM; 180 nM; 500 nM |
| 体内研究: |
JNJ-38158471 (10 or 100 mg/kg; p.o.; once-daily) inhibits VEGF-induced corneal neovascularization. JNJ-38158471 (10-200 mg/kg; p.o.) inhibits the growth of human tumor xenografts in a dose-dependent manner in both A431 and HCT116 models. JNJ-38158471 treatment is well tolerated, following continuous administration for 24 days, body weights were comparable with control animals. JNJ-38158471 (100 mg/kg; p.o.; once-daily) treatment shows statistically significant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end. |
| 参考文献: |
1. Kenneth RL, et, al. A Highly Selective, Orally Bioavailable, Vascular Endothelial Growth Factor receptor-2 Tyrosine Kinase Inhibitor Has Potent Activity in Vitro and in Vivo. Angiogenesis. 2009; 12(3): 287-96. |
| 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 |
2.741 ml |
13.707 ml |
27.413 ml |
| 5 mM |
0.548 ml |
2.741 ml |
5.483 ml |
| 10 mM |
0.274 ml |
1.371 ml |
2.741 ml |
| 50 mM |
0.055 ml |
0.274 ml |
0.548 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。 |