產(chǎn)品描述: | Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively. |
靶點: |
B-Raf:1 nM (Ki);B-RafV600E:1 nM (Ki);c-Raf:0.3 nM (Ki);Raf |
體外研究: |
Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers |
參考文獻: |
1. Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.088 ml |
10.44 ml |
20.88 ml |
5 mM |
0.418 ml |
2.088 ml |
4.176 ml |
10 mM |
0.209 ml |
1.044 ml |
2.088 ml |
50 mM |
0.042 ml |
0.209 ml |
0.418 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |