Catalog No.: PC-72620Not For Human Use, Lab Use Only.
PF-06821497 (PF 06821497) is a potent, selective, orally bioavailable Enhancer of Zeste Homolog 2 (EZH2) inhibitor with Ki of <1 nM against Y641N mutant.
PF-06821497 (PF 06821497) is a potent, selective, orally bioavailable Enhancer of Zeste Homolog 2 (EZH2) inhibitor with Ki of <1 nM against Y641N mutant.
PF-06821497 demonstrates high selectivity in the CEREP histone methyltransferase and broad-ligand screening panels, with exception EZH1 (Ki=70 nM), does not impair the function of various cytochrome P450 (CYPs) isoforms (IC50>30 uM) and does not exhibit appreciable inhibition of hERG ion channel.
PF-06821497 significantly reduced H3K27me3 levels in mice bearing Karpas-422 DLBCL tumor xenografts (which contain the Y641N EZH2 mutation).
