Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleosome assay).

Tazemetostat inhibits multi wild-type and mutant lymphoma cell lines proliferation (IC50s: 0.49 nM-7.6 μM).

Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) almost removes the fast-growing G401 tumors.

1403255-00-4

C34H47Cl3N4O4

682.12

EPZ-6438 trihydrochloride;E-7438 trihydrochloride;Tazemetostat trihydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years