PF-06726304 is a novel potent enhancer of zeste homolog 2 (EZH2) inhibitor with IC50 of <5 nM, Ki of 0.7/3.0 nM (Wt/Y641N).
PF-06726304 displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction (IC50=15 nM) and antiproliferation effect.
PF-06726304 also exhibits robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes.
