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Abiraterone Acetate

Abiraterone Acetate

产品编号 T6215   CAS 154229-18-2
别名: Zytiga, 乙酸阿比特龙酯, CB7630

Abiraterone Acetate (CB7630) 是一种具有口服活性的、不可逆的 CYP17A1选择性抑制剂,具有抗雄激素作用。它是 Abiraterone 的前药。

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Abiraterone Acetate Chemical Structure
Abiraterone Acetate, CAS 154229-18-2
规格 价格/CNY 货期 数量
5 mg ¥ 281 现货
10 mg ¥ 455 现货
50 mg ¥ 622 现货
100 mg ¥ 828 现货
500 mg ¥ 1,980 现货
1 mL * 10 mM (in DMSO) ¥ 490 现货
产品目录号及名称: Abiraterone Acetate (T6215)
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纯度: 99.83%
纯度: 99.51%
纯度: 99.51%
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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 Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.
靶点活性 CYP17:72 nM
体外活性 在啮齿动物模型中腹膜内给药后,发现Abiraterone具有快速脱乙酰化作用. 当作为其醋酸酯前药(CB7630)给药时,其抑制循环睾酮至检测不到的水平,并显著降低雄激素敏感器官的重量. Abiraterone具有良好的耐受性,实验中平均消除半衰期为27.6 h(因此可以每日一次给药).使用Abiraterone的临床前研究显示CYP17下游雄激素生成减少,导致小鼠腹侧前列腺,睾丸和精囊的重量减轻.
体内活性 Abiraterone抑制AR-阳性前列腺癌细胞的体外增殖和AR调控的基因表达,这可能是除了类固醇生成抑制作用外的AR拮抗作用造成的。Abiraterone阻断3β-羟化类固醇脱氢酶(3βHSD),这是一种合成生物活性雄激素所必需的酶。Abiraterone对3βHSD的抑制阻断DHT合成和雄激素受体响应。Abiraterone仅在SM1中表现出与血红素铁良好的络合作用。Abiraterone通过抑制CYP17A1,阻断雄激素的合成。Abiraterone抑制DHEA转化为Δ4-雄烯二酮。Abiraterone抑制Δ5-雄烯二醇转化为睾酮。Abiraterone在大鼠睾丸微粒体中抑制C17,20-裂解酶,IC50为5.8 nM。Abiraterone明显抑制睾酮分泌(-48%),进而增加LH浓度(192%)。
激酶实验 C17,20-lyase activity assay: Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contains 0.25 M sucrose, 20 mM Tris-HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, test compounds are evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at -20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format in our laboratory using a specific antibody against Δ4A and instructions provided by Biogenesis. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration.
细胞实验 LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence. (Only for Reference)
别名 Zytiga, 乙酸阿比特龙酯, CB7630
分子量 391.55
分子式 C26H33NO2
CAS No. 154229-18-2

存储

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

溶解度

DMSO: 3.92 mg/mL (10 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
DMSO 1 mM 2.554 mL 12.7698 mL 25.5395 mL 63.8488 mL
5 mM 0.5108 mL 2.554 mL 5.1079 mL 12.7698 mL
10 mM 0.2554 mL 1.277 mL 2.554 mL 6.3849 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. Pinto-Bazurco Mendieta MA, et al. J Med Chem. 2008, 51(16), 52009-52018. 2. Li R, et al. Clin Cancer Res. 2012, 18(13), 3571-3579. 3. Duc I, et al. J Steroid Biochem Mol Biol. 2003, 84(5), 537-542. 4. Richards J, et al. Cancer Res. 2012, 72(9), 2176-2182.

文献引用

1. Rice M A, Kumar V, Tailor D, et al. SU086, an inhibitor of HSP90, impairs glycolysis and represents a treatment strategy for advanced prostate cancer. Cell Reports Medicine. 2022: 100502. 2. Zhang X, Cheng L, Gao C, et al.Androgen Signaling Contributes to Sex Differences in Cancer by Inhibiting NF-κB Activation in T Cells and Suppressing Anti-Tumor Immunity.Cancer Research.2023
CYP1B1-IN-5 Beta-Tetralone Clopidogrel hydrogen sulfate α-​Terpinyl acetate Schizandrin A CYP1B1-IN-4 5,6,7-Trimethoxycoumarin Alizarin

相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 药物功能重定位化合物库 抗乳腺癌化合物库 FDA上市及药典收录分子库 口服活性化合物库 儿童药物库 FDA 上市药物库

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
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。
% DMSO
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% ddH2O
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

Abiraterone Acetate 154229-18-2 Metabolism P450 Zytiga inhibit CB 7630 CYPs Inhibitor Cytochrome P450 Abiraterone CB-7630 乙酸阿比特龙酯 CB7630 inhibitor

 

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