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Vorinostat

Vorinostat

产品编号 T1583   CAS 149647-78-9
别名: MK0683, 伏立诺他, suberoylanilide hydroxamic acid, SAHA

Vorinostat (suberoylanilide hydroxamic acid) 是一种具有抗肿瘤活性的组蛋白脱乙酰酶泛抑制剂,IC50值约为 10 nM。

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Vorinostat Chemical Structure
Vorinostat, CAS 149647-78-9
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
产品目录号及名称: Vorinostat (T1583)
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纯度: 99.93%
纯度: 99.47%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Vorinostat (suberoylanilide hydroxamic acid) 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 MK0683, 伏立诺他, suberoylanilide hydroxamic acid, SAHA
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 1 year

溶解度

Ethanol: 2 mg/mL(7.6 mM)

DMSO: 125 mg/mL (472.90 mM), Sonification is recommended

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Hrzenjak A et al. Histone deacetylase inhibitor vorinostat suppresses the growth of uterine sarcomas in vitro and in vivo. Mol Cancer. 2010 Mar 4;9:49. 2. Richon VM, et al. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):3003-7. 3. Munster PN, et al. The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces differentiation of human breast cancer cells. Cancer Res. 2001 Dec 1;61(23):8492-7. 4. Hockly E, et al. Suberoylanilide hydroxamic acid, a histone deacetylase inhibitor, ameliorates motor deficits in a mouse model of Huntington's disease. Proc Natl Acad Sci U S A. 2003 Feb 18;100(4):2041-6. 6. Wang J, et al. Snail determines the therapeutic response to mTOR kinase inhibitors by transcriptional repression of 4E-BP1. Nat Commun. 2017 Dec 20;8(1):2207. 7. Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity[J]. bioRxiv. 2021

文献引用

1. Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity. Cancer Immunology Research. 2022, 10(1): 87-107. 2. Wellinger L C, Hogg S J, Newman D M, et al. Bet inhibition enhances TNF-mediated antitumor immunity. Cancer Immunology Research. 2022, 10(1): 87-107 3. Yuting Meng,Xixi Qian,Li Zhao,Nan Li,Shengjie Wu,Baoan Chen,Tong Sun,Xuerong Wang Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma. Cancer Cell International. 2021, 21(1): 1-12. 4. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22. 5. Liang X L, Ouyang L, Yu N N, et al.Histone deacetylase inhibitor pracinostat suppresses colorectal cancer by inducing CDK5-Drp1 signaling-mediated peripheral mitofission.Journal of Pharmaceutical Analysis.2023 6. Du T, Hu X, Hou Z, et al.Re-expression of epigenetically silenced PTPRR by histone acetylation sensitizes RAS-mutant lung adenocarcinoma to SHP2 inhibition.Cellular and Molecular Life Sciences.2024, 81(1): 1-14.
ACY-738 mTOR/HDAC-IN-1 HCl ITSA-1 Belinostat TMP269 NT160 SP-2-225 Trichostatin A

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌药物库 抗癌上市药物库 抗癌活性化合物库 抗病毒库 抗乳腺癌化合物库 已知活性化合物库 抗胰腺癌化合物库 经典已知活性库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
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每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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计算 重置

技术支持

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。

Keywords

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

 

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