1191385-19-9

1191385-19-9 structure

Name: B-Raf inhibitor 1 (dihydrochloride)
Chemical Name: N1-(4-Chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-1,5-isoquinolinediamine dihydrochloride
CAS Number: 1191385-19-9
Molecular Formula: C₂₆H₂₁Cl₃N₈
Molecular Weight: 551.85800
Catalog: Research Areas Cancer
Create Date: 2018-11-24 16:45:30
Modify Date: 2024-02-01 07:11:49
B-Raf inhibitor 1 dihydrochloride 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.

Name	N1-(4-Chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-1,5-isoquinolinediamine dihydrochloride
Synonyms	B-Raf inhibitor 1 dihydrochloride B-Raf inhibitor 1 (dihydrochloride)

Description	B-Raf inhibitor 1 dihydrochloride 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.
Related Catalog	Research Areas >> Cancer
Target	B-Raf:1 nM (Ki) B-RafV600E:1 nM (Ki) c-Raf:0.3 nM (Ki)
In Vitro	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.