B-Raf inhibitor 1 dihydrochloride

Catalogue Number: B1173-APE

Manufacturer:	Apexbio
Molecular Formula:	C26H21Cl3N8
Type:	Kinase Inhibitors
Shipping Condition:	Blue Ice
Unit(s):	10 mg, 100 mg, 5 mg, 50 mg

Overview
Datasheets

Description

Description: B-Raf inhibitor 1 is an inhibitor of B-Raf kinase with IC50 values of 0.31µM and 0.72µM for cell proliferation, respectively in A375 and HCT116 [1].B-Raf is important in signal transduction and some mutant B-Raf occurs in cancer cells. The most common mutation of these is V600E, which makes B-Raf kinase constitutively active. B-Raf inhibitor 1 belongs to the type IIA inhibitors and binds to the DFG-out ATP-binding site of B-Raf. The selectivity of B-Raf inhibitor 1 is less than of other type inhibitors. Besides mutant B-Raf, it can also inhibit wild type B-Raf and other tyrosine kinase. In cells with wild type B-Raf, B-Raf inhibitor 1 can activate the RAF-MEK-ERK signaling pathway via Raf dimerization. The preclinical toxicity test shows B-Raf inhibitor 1 can induce hyperplasia in a mouse model [1, 2].References:[1] Wang X, Kim J. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.[2] Smith AL, DeMorin FF, Paras NA, Huang Q, Petkus JK, Doherty EM, Nixey T, Kim JL, Whittington DA, Epstein LF, Lee MR, Rose MJ, Babij C, Fernando M, Hess K, Le Q, Beltran P, Carnahan J. Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. J Med Chem. 2009 Oct 22;52(20):6189-92.

Additional Text

Storage Note

Store at -20°C

Smile String

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.Cl.Cl

Solubility

≥53.9 mg/mL in DMSO; ≥4.04 mg/mL in EtOH with ultrasonic; insoluble in H2O

B1173 Datasheet

B1173 CofA

B1173 MSDS

Price

£308.00

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