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Mocetinostat

Mocetinostat

产品编号 T2512   CAS 726169-73-9
别名: MGCD0103, MG0103

Mocetinostat (MG0103) 是一种可口服和同种型选择性的HDAC 抑制剂,抑制HDAC1,HDAC2,HDAC3和HDAC11的IC50分别为0.15,0.29,1.66 和 0.59 μM。

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Mocetinostat Chemical Structure
Mocetinostat, CAS 726169-73-9
规格 价格/CNY 货期 数量
1 mg ¥ 288 现货
5 mg ¥ 661 现货
10 mg ¥ 913 现货
25 mg ¥ 1,520 现货
50 mg ¥ 2,230 现货
100 mg ¥ 3,570 现货
200 mg ¥ 4,970 现货
500 mg ¥ 7,730 待询
1 mL * 10 mM (in DMSO) ¥ 661 现货
产品目录号及名称: Mocetinostat (T2512)
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纯度: 99.37%
纯度: 99.04%
纯度: 99%
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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 Mocetinostat (MG0103) is an orally available HDAC inhibitor with most potency for HDAC1 (IC50: 0.15 μM), 2- to 10- fold selectivity against HDAC2/3/11.
靶点活性 HDAC1:0.15 μM(cell free), HDAC11:0.59 μM(cell free), HDAC3:1.66 μM(cell free), HDAC2:0.29 μM(cell free)
体外活性 Mocetinostat (MGCD0103) potently targets human HDAC1 but also has inhibitory activity against HDAC2, HDAC3, and HDAC11 in vitro. In intact cells, MGCD0103 inhibited only a fraction of the total HDAC activity and showed long-lasting inhibitory activity even upon drug removal. MGCD0103 induced hyperacetylation of histones, selectively induced apoptosis, and caused cell cycle blockade in various human cancer cell lines in a dose-dependent manner [1]. MGCD0103 inhibited HDAC activity in several human cancer cell lines in vitro and in human peripheral WBC ex vivo in a dose-dependent manner. The HDAC inhibitory activity of MGCD0103 was time-dependent and sustained for at least 24 hours following drug removal in peripheral WBC ex vivo [2].
体内活性 In vivo, MGCD0103 significantly inhibited the growth of human tumor xenografts in nude mice in a dose-dependent manner and the antitumor activity correlated with the induction of histone acetylation in tumors [1]. Inhibitory activity of MGCD0103 was sustained for at least 8 hours in vivo in mice and 48 hours in patients with solid tumors. In cancer patients, sustained pharmacodynamic effect of MGCD0103 was visualized only by dose-dependent enzyme inhibition in peripheral WBC but not by histone acetylation analysis [2]. The 7-day intragastric administration of MGCD0103 with high dosage slightly induces the metabolism of tolbutamide in rat. MGCD0103 was not able to induce or inhibit the activity of CYP1A2, CYP2B1, CYP2D4, and CYP3A2 enzyme [3]. MGCD0103 improved pulmonary artery acceleration time and reduced systolic notching of the pulmonary artery flow envelope [4].
激酶实验 The deacetylase enzyme assay was based on a homogeneous fluorescence release assay. Purified recombinant HDAC enzymes were incubated with compounds diluted in various concentrations for 10 min in assay buffer [25 mmol/L HEPES (pH 8.0), 137 mmol/L NaCl, 1 mmol/L MgCl2, 2.7 mmol/L KCl] at room temperature. The substrate Boc-Lys(ε-Ac)-AMC was added to the reaction for further incubation at 37°C. The concentration of the substrate and the incubation time varied for different isotypes of HDAC enzymes. A 20-min trypsin incubation at room temperature allowed the release of the fluorophore from the deacetylated substrate. The fluorescent signal was detected by fluorometer at excitation of 360 nm, emission of 470 nm, and cutoff at 435 nm. The IC50 values of the compounds were determined by analyzing dose-response inhibition curves [1].
细胞实验 Cells were transfected with antisense oligonucleotides for 4 h everyday for 2 d. At 48 h after initial transfection, cells were harvested and apoptosis was evaluated with the Cell Death Detection ELISA Plus kit following the manufacturer's protocol. In all experiments, a fixed amount of DNA-histone complex, provided with the ELISA kit as a positive control, was used to ensure results were comparable among experiments. To analyze caspase-dependent apoptosis, an antibody specifically recognizing the caspase cleavage fragment of human poly(ADP-ribose) polymerase (PARP) was used to probe Western blots of lysates from cells treated with MGCD0103 [1].
动物实验 Female CD-1 nude mice, ages 8 to 10 wk, were used. Tumor fragments (~30 mg), which had been serially passaged thrice in vivo in minimal, were implanted s.c. through a small surgical incision on the flank of the mice while under general anesthesia. HDAC inhibitors were dissolved in vehicle (PBS acidified with 0.1 N HCl or PEG400/0.2 N HCl saline, 40:60) and dosed p.o. as solutions daily. Tumor volumes and body weight were monitored thrice weekly for at least 2 wk. Each experimental group contained six to eight animals. For pharmacokinetic study, blood was collected from animals at various time points, and plasma samples were analyzed using an HPLC system coupled with a triple quadrupole mass spectrometer [1]. . Forty rats (220 ± 20?g) were randomly divided into four different dosages of MGCD0103 groups (Low group, Medium group, High group, and control group with 10 rats in each group). MGCD0103 was dissolved in corn oil as suspension at three different concentrations (20, 40, and 80?mg/mL). Three different MGCD0103 groups (Low group, Medium group, and High group) were respectively given MGCD0103 20, 40, and 80?mg/kg one time by intragastric administration at every morning and last for 7 days. Control group were given saline by same administration method. At 8 days morning, six probe drugs, bupropion, phenacetin, tolbutamide, metoprolol, testosterone, and omeprazole, were mixed in corn oil and given to the rats of three MGCD0103 groups and control group by intragastric administration at a single dosage of 10?mg/kg for bupropion, phenacetin, metoprolol, testosterone, and omeprazole and 1?mg/kg for tolbutamide. Blood (0.3?mL) samples were collected into heparinized 1.5?mL polythene tubes from the tail vein at 0.0833, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, and 48?h after intragastric administration of six probe drugs. 100?μL of plasma was obtained from blood sample after centrifugation at 4000?g for 10?min. In a 1.5?mL centrifuge tube, 200?μL of acetonitrile (containing 50?ng/mL IS) was added into 100?μL of collected plasma sample. After vortex-mixing for 1.0?min, the sample was centrifuged at 13000?g for 15?min. Then supernatant (2?μL) was injected into the UPLC-MS/MS system for analysis. Concentration of plasma probe drugs versus time was analyzed by Version 3.0 Data Analysis System. The main pharmacokinetic parameters of the MGCD0103 group and control group were analyzed by SPSS l8.0 statistical software [3].
别名 MGCD0103, MG0103
分子量 396.44
分子式 C23H20N6O
CAS No. 726169-73-9

存储

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

溶解度

DMSO: 11 mg/mL (27.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5224 mL 12.6122 mL 25.2245 mL 63.0612 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL 12.6122 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL 6.3061 mL
20 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1531 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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参考文献

1. Fournel M, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68. 2. Bonfils C, et al. Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay. Clin Cancer Res. 2008 Jun 1;14(11):3441-9. 3. Cai J, et al. The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method. Biomed Res Int. 2015;2015:517295. 4. Cavasin MA, et al. Selective class I histone deacetylase inhibition suppresses hypoxia-induced cardiopulmonary remodeling through an antiproliferative mechanism. Circ Res. 2012 Mar 2;110(5):739-48.

文献引用

1. Zhao L, Huang C, Zheng R, et al. Photodynamic amplified immune checkpoint-blockade therapy of self-delivery bioregulator via epigenetic reprogramming. Chemical Engineering Journal. 2022: 139729.
HDAC-IN-52 BML-210 BRD4097 Bakkenolide A Tucidinostat mTOR/HDAC-IN-1 HCl BG45 CUDC-101

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌上市药物库 抗癌活性化合物库 药物功能重定位化合物库 肝脏毒性化合物库 经典已知活性库 上市药物库 染色质修饰分子库 DNA 损伤和修复分子库

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
mg/kg
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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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

Mocetinostat 726169-73-9 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases MGCD0103 inhibit MG0103 MGCD 0103 MGCD-0103 MG-0103 MG 0103 Inhibitor inhibitor

 

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