Chemical Structure : NVP-CGM097
CAS No.: 1313363-54-0
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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5 mg | ¥980 | In stock | |
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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.
分子量 | 659.27 | |
分子式 | C38H47ClN4O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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 |
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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