EPZ011989 hydrochloride

Based on 9 reference(s) in Google Scholar 8 10 9

Axon 4216

CAS [2095432-26-9]

MF C35H51N5O4.HCl
MW 641.26

  • Purity: 98%
  • Soluble in DMSO
Recently added

EPZ011989 hydrochloride

Description

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.

KEYWORDS: EPZ011989 hydrochloride | Supplier | EZH2 inhibitor | EPZ-011989 | EPZ 011989 | CT-EPZ989 | CAS [2095432-26-9] | [1598383-40-4] | Histone | HMTase | Inhibitor | Enzymes

Cell permeable, metabolically stable and orally available EZH2 inhibitor

Chemical name

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl((1r,4r)-4-((2-methoxyethyl)(methyl)amino)cyclohexyl)amino)-2-methyl-5-(3-morpholinoprop-1-ynyl)benzamide hydrochloride

Parent CAS No.

[1598383-40-4]

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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