伏立诺他 T1583

Product Introduction
Bioactivity


英文名: Vorinostat

描述: 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。

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].

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 2 mg/mL(7.6 mM)
DMSO : 125 mg/mL (472.90 mM)


关键字: Autophagy | Apoptosis | Filovirus | Histone deacetylases | Human papillomavirus | inhibit | HDAC | Inhibitor | Mitophagy | Vorinostat | MK 0683 | Mitochondrial Autophagy | HPV | MK-0683

相关产品: Edaravone | CA-5f | HFY-4A | Ramipril | Alisertib | L-Glutamic acid monosodium salt | Bz 423 | RA-9 | NS-1619 | B-AP15

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library | Anti-Infection Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途