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Chemical Structure : Tazemetostat
CAS No.: 1403254-99-8
Catalog No.: PC-21938Not For Human Use, Lab Use Only.
Tazemetostat (EPZ-6438) is a potent, selective, SMA-competitive and orally available EZH2 inhibitor with IC50 of 11 and 16 nM in peptide assay and nucleosome assay, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $118 | In stock | |
| 50 mg | $168 | In stock | |
| 100 mg | $248 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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Tazemetostat (EPZ-6438) is a potent, selective, SMA-competitive and orally available EZH2 inhibitor with IC50 of 11 and 16 nM in peptide assay and nucleosome assay, respectively.
Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with Ki of 2.5 nM, inhibits rat EZH2 with IC50 of 4 nM.
Tazemetostat (EPZ-6438) selectively inhibits intracellular lysine 27 of histone H3 (H3K27) methylation in a concentration- and time-dependent manner in both EZH2 wild-type and mutant lymphoma cells.
Tazemetostat (EPZ-6438) treatment causes dose-dependent tumor growth inhibition in EZH2-mutant NHL xenograft-bearing mice.
| M.Wt | 572.75 | |
| Formula | C34H44N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide |
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1. Knutson SK, et al. Mol Cancer Ther. 2014 Apr;13(4):842-54.
2. Knutson SK, et al. PLoS One. 2014 Dec 10;9(12):e111840.
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