Tazemetostat hydrobromide

Tazemetostat hydrobromide is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2) -containing wild-type EZH2 (Ki: 2.5 nM) . Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM) . (In Vitro) :Tazemetostat hydrobromide inhibits Rat EZH2 (IC50: 4 nM) . Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM . (In Vivo) :Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors .