EPZ011989 hydrochloride
- Parent CAS: 1598383-40-4
- Soluble in DMSO
- MF: C35H51N5O4.HCl
- MW: 641.26
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.
More Information
| Parent CAS No. | 1598383-40-4 |
|---|---|
| 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 |
| extra_info | Sold in collaboration with Chemietek |
| MFCD | N.A. |
| Short Description | EZH2 inhibitor |
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