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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 | Availability | Quantity |
---|---|---|---|
2 mg | $36 | In Stock | |
5 mg | $55 | In Stock | |
10 mg | $74 | In Stock | |
50 mg | $97 | In Stock | |
100 mg | $162 | In Stock | |
200 mg | $243 | In Stock | |
500 mg | $397 | In Stock | |
1 mL x 10 mM (in DMSO) | $76 | 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 | EZH1:392 nM, EZH2 (WT):2.5 nM (Ki), EZH2:11 nM (in peptide assay), EZH2:16 nM (in nucleosome assay), EZH2 (rat):4 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]. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (152.99 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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