EPZ011989

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.