TazemetoSTAT hydrobromide 是口服的EZH2选择性抑制剂。它抑制含有 PRC2 复合体的野生型 EZH2 的活性，Ki 为 2.5 nM。它还抑制 EZH1，IC50为 392 nM。

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).

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 [1].

Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors [1].

1467052-75-0

C34H45BrN4O4

653.65

氢溴酸泰泽司他;EPZ-6438 hydrobromide;E-7438 hydrobromide

DMSO:100 mg/mL (152.99 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years