PF-06821497

PF-06821497 is an enhancer of zeste homolog 2 (EZH2) inhibitor (Ki = <0. nM for EZH2Y641N). It is selective for EZH2 over a panel of 14 methyltransferases, 40 kinases, and 79 additional targets at 10 µM but does bind to EZH1 (Ki = 70 nM). PF-06821497 reduces trimethylation of lysine 27 on histone H3 (H3K27Me3) in, and the proliferation of, Karpas-422 non-Hodgkin lymphoma cells, which endogenously express EZH2Y641N (IC50s = 4 and 6 nM, respectively). In vivo, PF-06821497 (100 mg/kg, s.c.) induces tumor regression in a Karpas-422 mouse xenograft model.. Solulibility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml: DMSO: Slightly Soluble: 0.1-1 mg/ml, Water: Slightly Soluble: 0.1-1 mg/ml.