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Organic compounds that consist of sulfuric acid with organic functional group substitutions; includes compounds that are derived from organic sulfuric acids.
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NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor, demonstrating an IC50 of 1.7±0.1 nM for hMDM2. It is more potent than Nutlin-3a and effectively reactivates the p53 pathway in MDM2-amplified tumor models, selectively inhibiting the proliferation of cells expressing wild-type p53.
Binds to human MDM2 with high selectivity over MDM4.
More potent than Nutlin-3a.
Inhibits proliferation of cells expressing wild-type p53.
Redistributes wild-type p53 into the cell nucleus.
Reactivates p53 pathway in MDM2-amplified SJSA-1 human tumor models.
Inhibits SJSA-1 tumor growth in rats.
Well absorbed after oral dosing.
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