B-Raf inhibitor 1 |
| カタログ番号GC11599 |
B-Raf 阻害剤 1 は、B-RafWT、B-RafV600E、および C-Raf に対してそれぞれ 1 nM、1 nM、および 0.3 nM の Kis を持つ強力な Raf キナーゼ阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1093100-40-3
Sample solution is provided at 25 µL, 10mM.
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B-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.
B-Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. B-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. B-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[1].
References:
[1]. Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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