Valemetostat tosylate is a first-in-class dual EZH1/2 inhibitor with an IC50 value of less than 10 nM.Valemetostat tosylate is used in the study of relapsed/refractory peripheral T-cell lymphomas[1][2][3].In the concentration range of 1-1000 nM, Valemetostat tosylate strongly and specifically inhibits EZH1 and EZH2 with IC50 values of less than 10 nM[3].At a concentration of 100 nM for 7 days, Valemetostat tosylate effectively removed H3K27me3 and prevented unintended gain of H3K27me3[3].Valemetostat tosylate is effective in inhibiting H3K27me3 in sensitive lymphoma types at low doses over a 7-day period at concentrations ranging from 0.1-100 nM[3].
Valemetostat tosylate 动物研究
Animal study
Administered once intraperitoneally at a dose of 0.01 mg/g, Valemetostat tosylate prevented changes in H3K27me3 following exercise training in animals[2].
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