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B-Raf inhibitor 1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
B-Raf inhibitor 1图片
CAS NO:1093100-40-3
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
B-Raf inhibitor 1 是一种有效的 Raf 激酶抑制剂，对 B-RafWT、B-RafV600E 和 C-Raf 的 Kis 分别为 1 nM、1 nM 和 0.3 nM。
Cas No.1093100-40-3
别名N1-(4-氯苯基)-6-甲基-N5-[3-(9H-嘌呤-6-基)-2-吡啶]-1,5-异喹啉二胺
化学名1-N-(4-chlorophenyl)-6-methyl-5-N-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine
Canonical SMILESCC1=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
分子式C26H19ClN8
分子量478.94
溶解度≥ 47.9mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

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.