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