In Vitro: EPZ011989 inhibits mutant and wild-type EZH2 with an Ki value of <3 nM. EPZ011989 reduces cellular H3K27 methylation with an IC50 value of 94 nM. EPZ011989 (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells.
In Vivo: EPZ011989 (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity.