Biological Activity:CPI-169 is a highly potent and selective small molecule inhibitor of histone methyltransferase EZH2. It potently inhibits wild-type EZH2, mutant EZH2 Y641N and EZH1 with IC50 of 0.24 nM, 0.51 nM and 6.1 nM, respectively. It decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis across a large cell panel representing various non-Hodgkin’s lymphoma (NHL) subtypes. a variety of cell lines. Administered subcutaneously at 200 mpk twice daily (BID), CPI-169 is well tolerated in mice with no observed toxic effect or body weight loss. The drug treatment led to tumor growth inhibition (TGI) of an EZH2 mutant KARPAS-422 DLBCL xenograft. CPI-169 selectively affects the turnover of trimethylated, but not monomethylated histone H3 lysine 27 at pharmacologically relevant doses.How to Use:In vitro: CPI-169 was used at 10 µM final concentration in vitro and in cellular assays.In vivo: CPI-169 was subcutaneously (SC) dosed to mice bearing KARPAS-422 subcutaneous xenografts at 200 mg/kg twice per day. Reference:1. Bradley WD., et al. EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation. (2014) Chem Biol. 21(11):1463-75.
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