RGNCY-0054 (CPUY201112 HSP90 inhibitor)

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CPUY201112 is a novel potent inhibitor of Heat-shock protein 90 (HSP90).It binds to the HSP90 ATP-binding pocket with a kinetic dissociation constant of 27+2.3 nM .  It exhibits potent in vitro antiproliferative effects in a range of solid tumors.Treatment of MCF-7 cells with CPUY201112 results in cell cycle arrest and apoptosis through the wild type p53 pathway (IC50 0.624+0.05 mM/L). CPUY201112 also significantly synergises with Nutlin-3a to induce cancer cell apoptosis.  Furthermore, CPUY201112 significantly inhibited the growth of MCF-7 xenografts in nude mice without body weight loss. CPUY201112 has potential in treating wild-type p53 realted cancers.

Systematic Name:  (2,4-dihydroxy-5-isopropylphenyl)(2-ethoxy-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)methanone


Formula: C19H23N3O4

Mol Wt: 357.41

PMID:  26743233

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Tags: Cancer, Apoptosis, CPUY201112, Tumor, RGNCY-0054, HSP90, MCF, MCF-7, p53, Nutlin