Vorinostat
作者：齐岳
发布时间：2023-09-13
17:13:58
点击数：
产品名称：Vorinostat
产品描述：
| 产品描述 | Vorinostat is a pan-inhibitor of Histone Deacetylase with antineoplastic activity (IC50: ~10 nM). |
| 靶点活性 | HDAC:~10 nM (cell free) |
| 体外活性 | Vorinostat (SAHA) efficiently suppressed MES-SA cell growth at a low dosage (3 μM) already after 24 hours treatment. Decrease of cell survival was even more pronounced after prolonged treatment and reached 9% and 2% after 48 and 72 hours of treatment, respectively. Colony forming capability of MES-SA cells treated with 3 μM vorinostat for 24 and 48 hours was significantly diminished and blocked after 72 hours [1]. SAHA inhibits HDAC1 and HDAC3 activity in vitro. Treatment of cells in culture with SAHA results in a marked hyperacetylation of histone H4 [2]. The concentrations of SAHA of ≥2.5 μM caused profound growth arrest. The IC50 of 0.75 μM was calculated as 50% reduction in cell number after 120 h of continuous exposure to SAHA. Cell cycle analysis evaluated after 48 h exposure to SAHA showed an accumulation of cells predominantly in G1 at low concentrations (1.25 and 2.5 μM) [3]. |
| 体内活性 | Nude mice injected with 5 x 10^6 MES-SA cells were treated for 21 days with vorinostat (50 mg/kg/day) and, in comparison to placebo group, a tumor growth reduction of more than 50% was observed [1]. For comparison, 100 mg/kg SAHA in either HOP-β-CD or DMSO was administered to WT and R6/2 by single i.p. injection. It had no difference in the degree of histone acetylation between untreated WT and R6/2 mice. Significant increases in histone acetylation could be detected only on s.c. administration of 200 mg/kg [4]. |
| 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 | SAHA, 伏立诺他, suberoylanilide hydroxamic acid, MK0683 |
| 分子量 | 264.32 |
| 分子式 | C14H20N2O3 |
| CAS No. | 149647-78-9 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 2 mg/mL(7.6 mM)
DMSO: 125 mg/mL (472.90 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
