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Description: NVP-CGM097 (also known as CGM-097, CGM 097, CGM 097, NVP CGM097) is a novel, highly potent, orally bioavailable and selective MDM2 ( (human homolog of double minute 2) inhibitor with IC50 of 1.7+/-0.1 nM for hMDM2 and with anticancer activity. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway. Upon oral administration, p53/HDM2 interaction inhibitor CGM097 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited, which may result in the restoration of p53 signaling and, thus, the p53-mediated induction of tumor cell apoptosis.
References: J Med Chem. 2015 Aug 27; 58(16):6348-58; Neuroendocrinology. 2016 Nov 21.
Related CAS#:1313367-56-4 (NVP-CGM097 sulfate)
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