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首页-小分子抑制剂&激动剂-Apoptosis-MDM2-p53-NVP-CGM097
NVP-CGM097

Chemical Structure : NVP-CGM097

CAS No.: 1313363-54-0

NVP-CGM097 (CGM097)

货号: PC-24496Not For Human Use, Lab Use Only.

NVP-CGM097 is potent and selective MDM2 inhibitor with Ki of 1.3 nM (human MDM2, HDM2), inhibits p53-MDM2 protein-protein interaction with IC50 of 1.7 nM in TR-FRET assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NVP-CGM097 is potent and selective MDM2 inhibitor with Ki of 1.3 nM (human MDM2, HDM2), inhibits p53-MDM2 protein-protein interaction with IC50 of 1.7 nM in TR-FRET assays.
NVP-CGM097 is 16-fold more potent on human than dog MDM2 and 51- and 37-fold more potent on human than mouse and rat MDM2, respectively.
NVP-CGM097 binds to human MDM2 with an IC50 of 1.7 nM and shows high selectivity over MDM4.
NVP-CGM097 is about four times more potent than Nutlin-3a (IC50 = 8.0 nM).
NVP-CGM097 significantly redistribute wild-type p53 into the cell nucleus with an IC50 of 0.224 μM.
NVP-CGM097 significantly inhibited the proliferation of cells expressing wild-type p53, while sparing the p53 null cells.
NVP-CGM097 dose dependently and significantly inhibited SJSA-1 tumor growth in rats.

物理化学性质&存储条件

分子量 659.27
分子式 C38H47ClN4O4
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

(S)-1-(4-Chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-(methyl(((1r,4S)-4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl)methyl)amino)phenyl)-1,4-dihydroisoquinolin-3(2H)-one

参考文献

1. Jeay S, et al. Elife. 2015 May 12;4:e06498.

2. Holzer P, et al. J Med Chem. 2015 Aug 27;58(16):6348-58.

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