Valemetostat (tosylate)

Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values [1][2][3].

Product Specifications

CAS Number

[1809336-93-3]

Product Name Alternative

DS-3201 (tosylate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/valemetostat-tosylate.html

Purity

99.84

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(C1=CC=C(C)C=C1)(O)=O.CC2=C(O[C@@](C)([C@]3([H])CC[C@@H](N(C)C)CC3)O4)C4=C(Cl)C=C2C(NCC(C5=O)=C(C=C(C)N5)C)=O

Molecular Formula

C33H42ClN3O7S

Molecular Weight

660.22

Precautions

H302, H315, H319

References & Citations

[1]Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.|[2]Shimizu J, Kawano F. Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice. J Physiol. 2022 Jul;600 (14) :3331-3353.|[3]Yamagishi M, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019 Nov 19;29 (8) :2321-2337.e7.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

EZH1

Citation 01

Am J Pathol. 2025 Jun;195 (6) :1124-1140.|Protein Cell. 2025 Jun 20;16 (6) :439-457.|Cancer Res. 2025 May 15;85 (10) :1803-1818.|Cells. 2023 Dec 30;13 (1) :81.