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EPZ011989 is a cell permeable, metabolically stable and orally available EZH2 inhibitor, a compound with oral exposure and metabolic stability that is able to elicit robust methyl mark inhibition and antitumor activity. It binds potently and selectively to the mutant and wild-type EZH2 with Ki values < 3 nM, and highly selective over closely-related EZH1 (>15-fold selectivity) and 20 other histone methyltransferases (HMTs) (>3000-fold selectivity) tested. Demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with IC50s below 100 nM.
Catalog NO: CT-EPZ989
CAS NO: 1598383-40-4
Mol. Formula: C35H51N5O4 ∙HCl ∙ H2O
MW: 660.3
** in vivo Quality material, * >99.5% by HPLC, a recrystallized pale yellow powder (pic attached). Clean and impeccable, with a spot-on quantitative microanalysis. Bulk stock, same day shipping.