B-Raf inhibitor 1

Modify Date: 2024-01-02 18:42:11

Use of B-Raf inhibitor 1

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.

Name	1-N-(4-chlorophenyl)-6-methyl-5-N-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine
Synonym	More Synonyms

Description	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.
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.

L1E

B-Raf inhibitor 1

N-(4-Chlorophenyl)-6-methyl-N-[3-(1H-purin-6-yl)-2-pyridinyl]-1,5-isoquinolinediamine

1,5-Isoquinolinediamine, N-(4-chlorophenyl)-6-methyl-N-[3-(9H-purin-6-yl)-2-pyridinyl]-

3idp

pyridylpurine aminoisoquinoline,1

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Price: $132/10mM*1mLinDMSO

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