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Tazemetostat trihydrochloride

Name: Tazemetostat trihydrochloride
Brand: TargetMol
SKU: T15240
Rating: 4.5 (1 reviews)

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Catalog No. T15240Cas No. 1403255-00-4

Alias EPZ-6438 trihydrochloride, E-7438 trihydrochloride

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).

Tazemetostat trihydrochloride

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Catalog No. T15240Alias EPZ-6438 trihydrochloride, E-7438 trihydrochlorideCas No. 1403255-00-4

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,630	2-4 weeks	2-4 weeks
50 mg	$2,190	2-4 weeks	2-4 weeks
100 mg	$2,710	2-4 weeks	2-4 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

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, EZH1:392 nM, EZH2 (WT):2.5 nM （ki）, EZH2:11 nM （in peptide assay), EZH2:16 nM （in nucleosome assay)
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

Chemical Properties

Molecular Weight	682.12
Formula	C₃₄H₄₇Cl₃N₄O₄
Cas No.	1403255-00-4
Smiles	O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(C4CCOCC4)CC)=C1C)NCC5=C(C)C=C(C)NC5=O.Cl.Cl.Cl
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent 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 TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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