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K-RAS4B inhibitor Cmpd2

Chemical Structure : K-RAS4B inhibitor Cmpd2

CAS No.:

K-RAS4B inhibitor Cmpd2

货号: PC-24581Not For Human Use, Lab Use Only.

KRAS4B inhibitor Cmpd2 is a specific inhibitor of K-RAS4B, inhibtis the KRAS activation of BRAF with IC50 of 0.8 uM in coupled assays, and BLI Kd of <1 uM prenylated K-RAS4B in the presence of PS.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KRAS4B inhibitor Cmpd2 is a specific inhibitor of K-RAS4B, inhibtis the KRAS activation of BRAF with IC50 of 0.8 uM in coupled assays, and BLI Kd of <1 uM prenylated K-RAS4B in the presence of PS.
KRAS4B inhibitor Cmpd2 shows much affinity for the truncated, soluble GTPase domain of K-RAS determined by nuclear magnetic resonance (NMR) (Kd=700 uM).
Cmpd2 impairs the K-RAS4B interaction with the RBD of RAF on bilayers.
Cmpd2 inhibits BRAF activation by the prenylated form of the oncogenic K-RAS4B G12V mutant with EC50 of < 5 uM.

物理化学性质&存储条件

分子量 446.77
分子式 C21H21BrClN3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-bromo-N-((2R,4S)-2-(4-chlorobenzyl)piperidin-4-yl)-1H-indole-3-carboxamide

参考文献

1. Fang Z, et al. Cell Chem Biol. 2018 Nov 15;25(11):1327-1336.e4.

2. Jansen JM, et al. PLoS One. 2017 Apr 6;12(4):e0174706.

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