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Background Information:
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.
Reference:
1. J. E. Campbell, et al, EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity, ACS Med Chem Lett. 2015 Mar 4;6 (5):491-495*Clean and impeccable product, made for reproducible high quality research.
APIM050326: EPZ011989
CAS No.: 1598383-40-4.
Molecular Formula: C35H51N5O4 ?HCl ? H2O.
Molecular Weight: 660.3.
Purity: >99.5% purity (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis Report.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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