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Tazemetostat hydrobromide

Catalog No. T17002Cas No. 1467052-75-0
Alias EPZ-6438 hydrobromide, E-7438 hydrobromide

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).

Tazemetostat hydrobromide

Tazemetostat hydrobromide

Purity: 99.03%
Catalog No. T17002Alias EPZ-6438 hydrobromide, E-7438 hydrobromideCas No. 1467052-75-0
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 SizePriceAvailabilityQuantity
2 mg$36In Stock
5 mg$55In Stock
10 mg$74In Stock
50 mg$97In Stock
100 mg$162In Stock
200 mg$243In Stock
500 mg$397In Stock
1 mL x 10 mM (in DMSO)$76In Stock
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Purity:99.03%
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Product Introduction

Bioactivity
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 (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 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].
AliasEPZ-6438 hydrobromide, E-7438 hydrobromide
Chemical Properties
Molecular Weight653.65
FormulaC34H45BrN4O4
Cas No.1467052-75-0
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.5299 mL7.6494 mL15.2987 mL76.4935 mL
5 mM0.3060 mL1.5299 mL3.0597 mL15.2987 mL
10 mM0.1530 mL0.7649 mL1.5299 mL7.6494 mL
20 mM0.0765 mL0.3825 mL0.7649 mL3.8247 mL
50 mM0.0306 mL0.1530 mL0.3060 mL1.5299 mL
100 mM0.0153 mL0.0765 mL0.1530 mL0.7649 mL

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