store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EDO-S101 (Tinostamustine) 是一种泛 HDAC 抑制剂,IC50为 6 nM,对 HDAC1、HDAC2 和 HDAC3 的 IC50 值分别为 9、9 和 25 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 719 | 现货 | ||
2 mg | ¥ 1,070 | 现货 | ||
5 mg | ¥ 1,820 | 现货 | ||
10 mg | ¥ 2,650 | 待询 | ||
25 mg | ¥ 4,520 | 待询 | ||
50 mg | ¥ 6,330 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,960 | 现货 |
产品描述 | EDO-S101 (Tinostamustine) is a pan HDAC inhibitor with IC50 values of 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3 , respectively. |
靶点活性 | HDAC1:9nM, HDAC3:25 nM, HDAC2:9nM |
体外活性 | EDOS101 inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10 mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50 mg/kg. EDO-S101 triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initial in vitro experiments in HL60 cells shows an activation of the intrinsic pathway of apoptosis with cleavage of caspases 3, 9 and PARP and a marked reduction of anti-apoptotic proteins XIAP and Mcl-1. |
体内活性 | Intracellular HDAC inhibition of EDO-S101, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10 mg/kg and lasts for about 12-16 hours. Exposure to EDO-S101 causes a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt's lymphoma. Tumors of BL rapidly shrink or are completely eradicated after i.v. administration of EDO-S101. |
激酶实验 | EDO-S101 is dissolved in DMSO and added to the assay buffer solution. EDO-S101 dilutions of 5 μL of each dilution is added to 50 μL of the reaction mixture including the Fluor de Lys substrate and all of the enzymatic reactions are conducted in duplicate at 37oC for 30 minutes. After enzymatic reactions, 50 μL of 2xHDAC developer is added to each well and fluorescence intensity is measured[1]. |
别名 | Tinostamustine, Minomustine |
分子量 | 415.36 |
分子式 | C19H28Cl2N4O2 |
CAS No. | 1236199-60-2 |
store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
EDO-S101 1236199-60-2 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases Inhibitor Tinostamustine EDOS101 inhibit EDO S101 Minomustine EDO-S-101 EDO-S 101 inhibitor