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ChemicalBook Product Catalog Valemetostat

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Valemetostat NEW

$96.00 1mg

$197.00 5mg

$347.00 10mg

Min. Order
Purity99.08%
Cas No1809336-39-7
Supply Ability10g
Update time2024-11-18

TargetMol Chemicals Inc.

TargetMol Chemicals Inc.

3YR

United States

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Chemical Properties

Product Name	Valemetostat
CAS No	1809336-39-7
EC-No
Min. Order
Purity	99.08%
Supply Ability	10g
Release date	2024/11/18

Product Introduction

Bioactivity

名称	Valemetostat
描述	Valemetostat (DS-3201) is an EZH1/2 inhibitor that can be used to study relapsed/refractory peripheral T-cell lymphoma.
体外活性	METHODS: Valemetostat (DS-3201) was used to treat a group of malignant lymphoma cell lines derived from EZH1+ differentiated lymphocytes at low doses (0.1-100 nM), and the expression of H3K27me3 in sensitive lymphoma cells was observed. RESULTS valemetostat effectively inhibited H3K27me3 in sensitive lymphoma types, showing a targeted effect. [1] METHODS: The EZH inhibitor valemetostat (0.1-1000nM) was chemically screened and derivatized using half the maximal inhibitory concentration (IC50) of EZH1/2 and cellular H3K27me3. RESULTS valemetostat strongly and specifically inhibits EZH1 and EZH2 (IC50 < 10 nM). [2] METHODS: Human MCL cell lines Mino, JeKo-1, and REC-1 were treated with varying concentrations of valemetostat ranging from 3000 to 0.3 nmol/L or 3000 to 100 nmol/L, respectively. RESULTS Valemetostat at a concentration lower than 100 nmol/L significantly inhibited the growth of Mino and JeKo-1, while valemetostat at a concentration higher than 100 nmol/L inhibited the growth of REC-1. [3]
体内活性	METHODS: In diffuse large B-cell lymphoma (DLBCL) cell xenograft model mice, Valemetostat (DS-3201) (25 mg/kg/50 mg/kg/100 mg/kg) was orally administered once a day to observe the tumor growth in the mice. RESULTS Valemetostat 100 mg/kg orally once daily was associated with nearly complete tumor regression without weight loss; lower doses (25 mg/kg) slowed tumor growth. [1] METHODS: Primary MCL cells were transplanted into 6-week-old SCID-Beige (SCIDbg) mice (CB17.Cg-Prkdc) by subcutaneous injection, and the mice were treated with valemetostat 200 mg/kg twice daily for three days. week. RESULTS valemetostat treatment significantly inhibited tumor growth, and all valemetostat-treated mice survived to the end of the study period. [3]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 45 mg/mL (92.21 mM)
关键字	Valemetostat \| inhibit \| Histone Methyltransferase \| DS 3201 \| Inhibitor \| T-cell \| DS3201 \| lymphoma
相关产品	BIX-01294 trihydrochloride \| Tazemetostat \| Piribedil \| XY1 \| UNC 0631 \| GSK126 \| MAK683 \| EZM 2302 \| EPZ015666 \| AMI-1 free acid \| MS37452 \| MRTX-1719
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