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EPZ-6438 is an inhibitor of EZH2, a histone methyltransferase (HMT) responsible for methylation of lysine and arginine residues and controls gene transcription fidelity in cells. EPZ-6438 displays anticancer chemotherapeutic activity in in vivo models by inducing regression of malignant or atypical teratoid rhabdoid tumors containing altered or mutant SWI/SNF ATP-dependent chromatin remodelers.
| Cas No. | 1403254-99-8 |
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| Purity | ≥98% |
| Formula | C34H44N4O4 |
| Formula Wt. | 572.74 |
| Chemical Name | N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide |
| IUPAC Name | N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide |
| Synonym | E7438, Tazemetostat, |
| Solubility | DMSO 5 mg/mL warmed (8.72 mM) Water Insoluble Ethanol Insoluble |
| Appearance | white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet | |
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Knutson SK, Warholic NM, Wigle TJ, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. PMID: 23620515.