Valemetostat tosylate

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Chemical Structure| 1809336-93-3 同义名 : DS-3201 tosylate
CAS号 : 1809336-93-3
货号 : A1216638
分子式 : C33H42ClN3O7S
纯度 : 99%+
分子量 : 660.22
MDL号 : MFCD32197179
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(159.04 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.51mL

0.30mL

0.15mL

7.57mL

1.51mL

0.76mL

15.15mL

3.03mL

1.51mL
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.

[3]Yamagishi M, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019 Nov 19;29(8):2321-2337.e7.