EPZ011989,EPZ-011989 purchase from DC Chemicals

EPZ011989,EPZ-011989 purchase from DC Chemicals
DC Chemicals provides EPZ011989, other names: EPZ011989,EPZ-011989, cas: 1598383-40-4. In stock.

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EPZ011989 is a potent, orally-available EZH2 Inhibitor.

EPZ011989, other names: EPZ011989,EPZ-011989, cas: 1598383-40-4, Molecule formular: , Molecule Weight: , Chemical name:

EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.EPZ011989, that equipotently inhibits mutant and wild-type EZH2 with an inhibition constant (Ki) of <3 nM. EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. As evidenced by the human and rat liver microsomal turnover, EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM.EPZ011989 is a compound with oral exposure and metabolic stability that is able to elicit robust methyl mark inhibition and antitumor activity.