产品描述: | SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases. |
靶点: |
B-Raf:0.16 nM (Ki);c-Raf:1.72 nM (Ki);Raf |
体内研究: |
Administration of SB-590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth |
参考文献: |
1. King AJ, et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res, 2006, 66(23), 11100-11105. 2. Takle AK, et al. The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett, 2006, 16(2), 378-381. 3. Smalley KS, et al. Increased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomas. Mol Cancer Ther, 2008, 7(9), 2876-2883. |
溶解性: |
DMSO : 33.33 mg/mL (73.49 mM; Need ultrasonic) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.205 ml |
11.024 ml |
22.049 ml |
5 mM |
0.441 ml |
2.205 ml |
4.41 ml |
10 mM |
0.22 ml |
1.102 ml |
2.205 ml |
50 mM |
0.044 ml |
0.22 ml |
0.441 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。 |