Valemetostat tosylate salt form · tosylate · Parent Valemetostat

Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM.

For research use only. Not for human or veterinary use.

Target Histone Methyltransferase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Valemetostat tosylate structure

CAS No.: 1809336-93-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 560.00	BP-02146A-50mg	In stock	Get quote
100 mg	USD 870.00	BP-02146A-100mg	In stock	Get quote
250 mg	USD 1,750.00	BP-02146A-250mg	In stock	Get quote
500 mg	USD 2,800.00	BP-02146A-500mg	In stock	Get quote

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BP-02146 — Valemetostat

Description

Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma[1][2][3].

Biological activity

In Vitro Valemetostat tosylate (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC50 values ＜10 nM. ? Valemetostat tosylate (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3. ? Valemetostat tosylate (0.1-100 nM; 7 d) potently inhibits H3K27me3 by low-dose treatment? in the sensitive lymphoma types. In Vivo Valemetostat tosylate (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training.

Identifiers

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
InChIKey: JSBKGJUYSLVFPF-WJQUPPJOSA-N

Specifications

MW (average): 660.2200
Formula: C₃₃H₄₂ClN₃O₇S
CAS No.: 1809336-93-3
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4°C, sealed storage, away from moisture; In solvent -20°C, 1 month;

Solubility

soluble in DMSO

Documents

References

[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.

Same target

Search Histone Methyltransferase

Same research area

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