RG7112，50MG，SML4102-50MG，Sigma

Biochem/physiol Actions

Orally active, potent and selective MDM2 inhibitor with anti-cancer efficacy in cultures and in vivo by induces p53-dependent cell cycle arrest and apoptosis.
RG7112 is an orally active, potent and selective MDM2 inhibitor that binds and blocks p53-binding site (IC50 = 18 nM), thereby induces p53-dependent cell cycle arrest and apoptosis (av GI50 by MTT assays = 0.4 μM/wt 53 vs 33.4 μM/mutant p53) by stabilizing cellular p53. When administered in vivo, RG7112 is efficacious against the growth of tumor xenografts in mice (SJSA-1, SJSA-1luc2, and MHM; 25-200 mg/kg via daily p.o.).