Valemetostat tosylate|1809336-93-3|-陌孚医药/Medlife

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Valemetostat tosylate

目录号: PL15052 纯度: ≥98%

CAS No. :1809336-93-3

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中文名称	Valemetostat tosylate
英文名称	Valemetostat tosylate
英文别名	Valemetostat (tosylate);6N79I7X5II;Valemetostat tosylate;1,3-Benzodioxole-5-carboxamide, 7-chloro-N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-2-(trans-4-(dimethylamino)cyclohexyl)-2,4-dimethyl-, (2R)-, compd. with 4-methylbenzenesulfonate (1:1);(R)-7-Chloro-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-((1r,4R)-4-(dimethylamino)cyclohexyl)-2,4-dimethylbenzo[d][1,3]dioxole-5-carboxamide 4-methylbenzenesulfona;DS-3201 tosylate
Cas No.	1809336-93-3
分子式	C₃₃H₄₂ClN₃O₇S
分子量	660.22
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Valemetostat tosylate (DS-3201 tosylate) 是一种首创的 EZH1/2 抑制剂，IC₅₀ 值＜10 nM。Valemetostat tosylate 可用于复发以及难治型周围 T 细胞淋巴瘤的研究。

生物活性

Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC 50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

性状

Solid

IC50 & Target[1][2]

EZH1

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Valemetostat tosylate (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J mice with chronic

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (151.46 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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