>>Signaling Pathways>> MAPK Signaling>> Raf>>B-Raf inhibitor 1 dihydrochloride

B-Raf inhibitor 1 dihydrochloride

Catalog No.GC14907

B-B-Raf 억제제 1 디히드로클로라이드는 B-RafWT, B-RafV600E 및 C-Raf에 대해 각각 1nM, 1nM 및 0.3nM의 Kis를 갖는 강력한 Raf 키나제 억제제입니다.

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B-Raf inhibitor 1 dihydrochloride Chemical Structure

Cas No.: 1191385-19-9

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 1191385-19-9 SDF
Chemical Name 1-N-(4-chlorophenyl)-6-methyl-5-N-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine;dihydrochloride
Canonical 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.Cl.Cl
Formula C26H21Cl3N8 M.Wt 551.86
Solubility DMF: 1mg/mL,DMSO: 10mg/mL,DMSO:PBS (pH 7.2) (1:2): 0.3mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.8121 mL 9.0603 mL 18.1205 mL
5 mM 0.3624 mL 1.8121 mL 3.6241 mL
10 mM 0.1812 mL 0.906 mL 1.8121 mL
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Review for B-Raf inhibitor 1 dihydrochloride

Average Rating: 5 ★★★★★ (Based on Reviews and 8 reference(s) in Google Scholar.)

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