PF-06726304|cas 1616287-82-1

PF-06726304|cas 1616287-82-1

DC Chemicals, Website:www.dcchemicals.com

Product Name: PF-06726304|CAS: 1616287-82-1|Cat No: DC10634|Other Names:

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.

In vitro:
PF-06726304 displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction and antiproliferation effect.
In vivo: PF-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.