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Tazemetostat hydrobromide

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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

😃Good
Purity: 99.8%
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$36In StockIn Stock
5 mg$55In StockIn Stock
10 mg$74In StockIn Stock
50 mg$97In StockIn Stock
100 mg$162In StockIn Stock
200 mg$243In StockIn Stock
500 mg$397-In Stock
1 mL x 10 mM (in DMSO)$76In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.8%
Appearance:Solid
Color:White
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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
EZH2:11 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].
SynonymsEPZ-6438 hydrobromide, E-7438 hydrobromide
Chemical Properties
Molecular Weight653.65
FormulaC34H45BrN4O4
Cas No.1467052-75-0
SmilesO=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 & Solubility Information
StoragePowder: -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
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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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

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