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B-Raf inhibitor 1 CAS: 1093100-40-3

Category: Inhibitors
Product Name: B-Raf inhibitor 1
Cat No: I000391
CAS No: 1093100-40-3
Synonyms: 1-N-(4-chlorophenyl)-6-methyl-5-N-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine
Molecular Formula: C26H19ClN8
Molecular Weight: 478.94
SMILES: CC1=C(C2=C(C=C1)C(=NC=C2)NC3=CC=C(C=C3)Cl)NC4=C(C=CC=N4)C5=C6C(=NC=N5)N=CN6
InChI: None
InChIKey: None
Solubility: DMSO: ≥ 53 mg/mL
Target: Raf
IC50: 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK [1]
Storage: Store at -20°C
CAS 1093100-40-3,B-Raf inhibitor 1
  • Description

B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.
IC50 value: 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK [1]
Target: B-Raf
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. Compound 13 exhibit 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. Compound 13 induced proliferation and hyperplasia in normal tissues of mice [1]

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


[1]. Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.


price inquiry for CAS:1093100-40-3, Product:B-Raf inhibitor 1