化学性质:
规格 | 5mg 10mg 50mg 100mg |
CAS | 1191385-19-9 |
别名 |
|
化学名 | 1-N-(4-chlorophenyl)-6-methyl-5-N-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine;dihydrochloride |
分子式 | C26H21Cl3N8 |
分子量 | 551.86 |
溶解度 | DMF: 1mg/mL,DMSO: 10mg/mL,DMSO:PBS (pH 7.2) (1:2): 0.3mg/mL |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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].
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