EZH1/2 抑制剂;EZH1/2 Inhibitors;;InformationPF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.TargetsEzh2 (wild-type) (cell-free); EZH2 Y641N (cell-free) 0.7 nM(Ki); 3 nM(Ki)In vitroPF-06726304 displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction and antiproliferation effect.In vivoPF-06726304 displays robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes. PF-06726304 displays good efficacy in a diffuse large B-cell lymphoma Karpas-422 tumor model and exhibited on-target pharmacodynamic effects in vivo.Cell Research(from reference)Cell lines:Karpas-422 cell line Incubation Time:72 h