Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 nucleosome assay). |
Targets&IC50 | EZH2 (rat):4 nM, EZH2:11 nM (in peptide assay), EZH2:16 nM (in nucleosome assay), EZH2 (WT):2.5 nM (ki), 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. |
Synonyms | EPZ-6438 trihydrochloride, E-7438 trihydrochloride |
Molecular Weight | 682.12 |
Formula | C34H47Cl3N4O4 |
CAS No. | 1403255-00-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Tazemetostat trihydrochloride 1403255-00-4 Chromatin/Epigenetic Histone Methyltransferase EPZ 6438 Trihydrochloride Tazemetostat E7438 EPZ-6438 Trihydrochloride EPZ-6438 EPZ-6438 trihydrochloride EPZ6438 Trihydrochloride E 7438 EPZ 6438 EPZ6438 E-7438 trihydrochloride E7438 Trihydrochloride E-7438 Trihydrochloride Tazemetostat Trihydrochloride E 7438 Trihydrochloride E-7438 inhibitor inhibit