Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vorinostat (SAHA) 是一种泛的组蛋白脱乙酰酶 (HDAC) 抑制剂 (IC50=10 nM),对 HDAC1/2/3/6/7/11 均有抑制活性。 Vorinostat 具有抗肿瘤活性,可以诱导细胞分化,阻滞细胞周期,诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 326 | 现货 | ||
200 mg | ¥ 817 | 现货 | ||
500 mg | ¥ 1,223 | 现货 | ||
1 g | ¥ 1,785 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 134 | 现货 |
产品描述 | Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1/2/3/6/7/11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis. |
靶点活性 | HDAC:~10 nM (cell free) |
体外活性 |
方法:滑膜肉瘤细胞 SW-982 和软骨肉瘤细胞 SW-1353 用 Vorinostat (0.5-15 μM) 处理 48 h,使用 MST assay 检测细胞活力。 结果:Vorinostat 以剂量依赖的方式抑制 SW-982 和 SW-1353 细胞增殖,IC50 分别为 8.6 μM 和 2.0 μM。[1] 方法:子宫肉瘤细胞 MES-SA 用 Vorinostat (3 μM) 处理 24-72 h,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:在整个处理期间,HDAC1 的表达没有差异。HDAC2、3 和 7 显示出 Vorinostat 对表达的显著抑制。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Vorinostat (50 mg/kg in HOP-β-CD) 腹腔注射给携带子宫肉瘤 MES-SA 的 Nude-Foxn1nu/nu 小鼠,每周五次,持续二十一天。 结果:与安慰剂组相比,Vorinostat 治疗组观察到肿瘤生长减少了 50% 以上。[1] 方法:为研究在真性红细胞增多症 (PV) 动物模型中的作用,将 Vorinostat (200 mg/kg in 50% PEG-400) 腹腔注射给 MxCre;Jak2V617F/+ 小鼠,每周五次,持续两周。 结果:Vorinostat 治疗使 Jak2V617F 敲除小鼠的外周血计数正常化,并显著减少脾肿大。Vorinostat 可能对 PV 和其他 JAK2V617F 相关的骨髓增生性肿瘤具有治疗潜力。[3] |
细胞实验 | Cells were plated onto 100-mm tissue culture plates at a density of 2 × 10^6 for 48 h and then treated with SAHA or equal concentrations of the vehicle. For longer drug exposure times, medium with drug or vehicle were exchanged every 48 h. For wash-out experiments, cells were treated with SAHA daily for 60–72 h (drug and medium were exchanged at 48 h), then SAHA was washed out and replaced with 10% FCS containing DMEM [3]. |
动物实验 | Athymic Nude-Foxn1nu/nu mice were used in the present study. They were housed at 22°C at a constant light-dark cycle (12-h light, 12-h dark) and had free access to water and rodent chow (4-5% fat, 21% protein). Twelve weeks old male mice (n = 14) were anesthetized with Isofluran and 5 × 10^6 MES-SA cells were injected subcutaneously into the right flank of the animal. Mice from a control group received placebo containing 300 μl of empty HOP-β-CD (2-hydroxypropyl-β-cyclodextrin) vesicles. Another group of mice received vorinostat dissolved in HOP-β-CD at a concentration of 50 mg/kg/day. Both, empty vesicles and vorinostat were administered intraperitoneally, starting on the day 4 after the injection of MES-SA tumor cells. Mice body weight and tumor size (w2 × l × 0.52; measured by caliper) were estimated twice a week. All mice were treated for 21 days and afterward sacrificed by cervical dislocation. Each tumor was isolated as a whole and different tumor parameters (weight, volume, size, and macroscopic appearance) were determined. Finally, tumor slices were cryopreserved and formalin fixed (4%) for further analyses [1]. |
别名 | MK0683, 伏立诺他, suberoylanilide hydroxamic acid, SAHA |
分子量 | 264.32 |
分子式 | C14H20N2O3 |
CAS No. | 149647-78-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 2 mg/mL(7.6 mM)
DMSO: 125 mg/mL (472.90 mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.7833 mL | 18.9165 mL | 37.8329 mL | 94.5823 mL |
5 mM | 0.7567 mL | 3.7833 mL | 7.5666 mL | 18.9165 mL | |
DMSO | 10 mM | 0.3783 mL | 1.8916 mL | 3.7833 mL | 9.4582 mL |
20 mM | 0.1892 mL | 0.9458 mL | 1.8916 mL | 4.7291 mL | |
50 mM | 0.0757 mL | 0.3783 mL | 0.7567 mL | 1.8916 mL | |
100 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9458 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。
Vorinostat 149647-78-9 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Microbiology/Virology Mitophagy Virus Protease HDAC MK0683 Filovirus Histone deacetylases 伏立诺他 suberoylanilide hydroxamic acid Human papillomavirus inhibit Inhibitor MK 0683 SAHA Mitochondrial Autophagy HPV MK-0683 inhibitor