Valemetostat
目录号: PL15038 纯度: ≥99%
CAS No. :1809336-39-7
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中文名称
Valemetostat
英文名称
Valemetostat
英文别名
Valemetostat;60RD0234VE;Valemetostat [INN]
Cas No.
1809336-39-7
分子式
C26H34ClN3O4
分子量
488.02
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
Valemetostat (DS-3201) 是一种首创的 EZH1/2 抑制剂,IC50 值 <10 nM。Valemetostat 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), a first-in-class EZH1/2 dual inhibitor with IC 50 values <10 nM. Valemetostat 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 (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC50 values <10 nM.
Valemetostat (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3.
Valemetostat (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 (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 and acut
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
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 : 70 mg/mL (143.44 mM; Need ultrasonic)配制储备液
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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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