Valemetostat (DS-3201)

Catalog No.S8926 Synonyms: DS-3201b

For research use only.

Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.

Valemetostat (DS-3201) Chemical Structure

CAS No. 1809336-39-7

Purity & Quality Control

Choose Selective EZH1/2 Inhibitors

Biological Activity

Description Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.
EZH1 [1] EZH2 [1]
In vitro

Valemetostat significantly reducs ATL cell viability compared with the others. Valemetostat significantly reactivates the expression of the highly H3K27me3-accumulated EZH1/2 target genes in an ex vivo culture of primary ATL cells. Valemetostat shows superior anti-growth effects compared with EZH2-selective inhibitor in malignant lymphoma cell lines.[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 488.02



CAS No. 1809336-39-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C(=O)N1)CNC(=O)C2=CC(=C3C(=C2C)OC(O3)(C)C4CCC(CC4)N(C)C)Cl)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04842877 Recruiting Drug: Valemetostat tosylate Lymphoma B-Cell The Lymphoma Academic Research Organisation|Daiichi Sankyo Inc. June 11 2021 Phase 2
NCT04703192 Recruiting Drug: Valemetostat Tosylate Relapsed/Refractory Peripheral T-Cell Lymphoma|Adult T Cell Leukemia/Lymphoma Daiichi Sankyo Inc. June 3 2021 Phase 2
NCT04276662 Completed Drug: DS-3201b Hepatic Impairment Daiichi Sankyo Inc. November 21 2019 Phase 1
NCT02732275 Active not recruiting Drug: DS-3201b Lymphoma Malignant|Non-hodgkin Lymphoma Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. March 31 2016 Phase 1

(data from, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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