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Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $36 | In Stock | In Stock | |
| 5 mg | $55 | In Stock | In Stock | |
| 10 mg | $74 | In Stock | In Stock | |
| 50 mg | $97 | In Stock | In Stock | |
| 100 mg | $162 | In Stock | In Stock | |
| 200 mg | $243 | In Stock | In Stock | |
| 500 mg | $397 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $76 | In Stock | In Stock |
| Description | Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM). |
| Targets&IC50 | EZH2:11 nM (in peptide assay), EZH2 (rat):4 nM, EZH2:16 nM (in nucleosome assay), EZH2 (WT):2.5 nM (Ki), EZH1:392 nM |
| In vitro | Tazemetostat hydrobromide inhibits Rat EZH2 (IC50: 4 nM). Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM [1]. |
| In vivo | Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors [1]. |
| Synonyms | EPZ-6438 hydrobromide, E-7438 hydrobromide |
| Molecular Weight | 653.65 |
| Formula | C34H45BrN4O4 |
| Cas No. | 1467052-75-0 |
| Smiles | O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O.[H]Br |
| Relative Density. | 1.31g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 102 mg/mL (156.05 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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