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Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleosome assay).
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Description | Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo |
Targets&IC50 | EZH2 (WT):2.5 nM (ki), EZH2:11 nM (in peptide assay), EZH2:16 nM (in nucleosome assay), EZH2 (rat):4 nM, EZH1:392 nM |
In vitro | Tazemetostat inhibits multi wild-type and mutant lymphoma cell lines proliferation (IC50s: 0.49 nM-7.6 μM). |
In vivo | Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) almost removes the fast-growing G401 tumors. |
Alias | EPZ-6438 trihydrochloride, E-7438 trihydrochloride |
Molecular Weight | 682.12 |
Formula | C34H47Cl3N4O4 |
Cas No. | 1403255-00-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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