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-classEZH1/2dual inhibitor withIC50values <10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma[1][2][3]. |
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体外研究 (In Vitro) | Valemetostat tosylate (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC50values <10 nM[3].Valemetostat tosylate (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3[3].Valemetostat tosylate (0.1-100 nM; 7 d) potently inhibits H3K27me3 by low-dose treatment in the sensitive lymphoma types[3].
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体内研究 (In Vivo) | Valemetostat tosylate (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training[2].
Animal Model: | Male C57BL/6J mice with chronic and acute running exercise or without exercise[1] | Dosage: | 0.01 mg/g | Administration: | Intraperitoneal injection; 0.01 mg/g; 30 min before the start of running exercise | Result: | Significantly increased the level of H3K27me3 , slightly decresed EZH1 level , upregulated the EZH2 level and increased the level of phosphorylated AMPK after exercise. Repressed myonuclear H3K27me3 accumulation during training and caused a failure of adaptive changes. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(151.46 mM;Need ultrasonic) 配制储备液 1 mM | 1.5146 mL | 7.5732 mL | 15.1465 mL | 5 mM | 0.3029 mL | 1.5146 mL | 3.0293 mL | 10 mM | 0.1515 mL | 0.7573 mL | 1.5146 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.15 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.15 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.15 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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