Cat No:LP000402
Product Name:EPZ-6438;Tazemetostat;E-7438
CAS#1403254-99-8
EPZ-6438 inhibits EZH2 in a manner competitive with the substrate S-adenosylmethionine (SAM). EPZ-6438 inhibits EZH1, EZH2(in peptide assay), EZH2 (in nucleosome assay) with IC50of 392 nM, 11 nM and 16 nM, respectively. EPZ-6438 displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs tested[1].
EPZ-6438 (125 mg/kg) induces tumor stasis during the administration period and produced a significant tumor growth delay compared with vehicle after the dosing period. Measuring EPZ-6438 plasma levels either 5 min before or 3 h after dosing on day 21 reveals a clear dose-dependent increase in systemic exposure[1]. Dose-dependent target inhibition is observed in PBMCs and bone marrow from rats dosed with EPZ-6438 (orally administered, 100, 300, or 1,000 mg/kg) as measured by ELISA.
