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Abiraterone

Abiraterone

产品编号 T6216   CAS 154229-19-3
别名: 阿比特龙, CB-7598

Abiraterone (CB-7598) 是不可逆的CYP17A1抑制剂,具有抗雄激素作用,抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶 (IC50:2.5 nM) 和 17,20-裂合酶 (IC50:15 nM) 活性。

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Abiraterone Chemical Structure
Abiraterone, CAS 154229-19-3
规格 价格/CNY 货期 数量
10 mg ¥ 398 现货
50 mg ¥ 1,169 现货
100 mg ¥ 1,775 现货
200 mg ¥ 2,366 现货
500 mg ¥ 3,990 现货
1 g ¥ 5,790 现货
产品目录号及名称: Abiraterone (T6216)
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纯度: 99.87%
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 Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).
靶点活性 CYP17:2 nM
体外活性 Abiraterone对睾丸激素水平的降低效果几乎切除睾丸的效果相同.Abiraterone对任何器官尺寸均无明显降低作用.Abiraterone可抑制人类睾丸微粒体中CYP17(IC50:72 nM).与对照组相比,Abiraterone 降低 95%以上睾丸激素水平.
体内活性 Abiraterone抑制体外增殖和雄激素受体调节的雄激素受体阳性前列腺癌细胞基因表达,这可能是通过抑制类固醇和抗雄激素受体实现的。更高浓度的Abiraterone抑制依普利酮激活的突变型雄激素受体。Abiraterone 取代WT-AR(EC50:13.4 μM)和T877A(EC50:7.9 μM)中的配体。Abiraterone醋酸盐明显抑制T分泌(48%),且可使LH浓度达到192%。Abiraterone抑制大鼠睾丸微粒的裂解酶活性(IC50:5.8 nM)。
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 contained 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, Abiraterone is 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 using a specific antibody against Δ4A. 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 1450 MicrobetaPlus 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 阿比特龙, CB-7598
化合物与蛋白结合的复合物

T6216_2

Zebra fish cytochrome P450 17A2 with Abiraterone

分子量 349.51
分子式 C24H31NO
CAS No. 154229-19-3

存储

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

溶解度

Ethanol: 5.4 mg/mL (15.45 mM), sonification is recommended.

DMF: 8.75 mg/mL (25.04 mM), sonification/heating is recommended.

DMSO: 5 mg/mL (14.31 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 / DMF / DMSO 1 mM 2.8611 mL 14.3057 mL 28.6115 mL 71.5287 mL
5 mM 0.5722 mL 2.8611 mL 5.7223 mL 14.3057 mL
10 mM 0.2861 mL 1.4306 mL 2.8611 mL 7.1529 mL
DMF 20 mM 0.1431 mL 0.7153 mL 1.4306 mL 3.5764 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. Attard G, et al. J Clin Oncol. 2008, 26(28), 4563-4571. 2. Richards J, et al. Cancer Res. 2012, 72(9), 2176-2182. 3. Duc I, et al. J Steroid Biochem Mol Biol. 2003, 84(5), 537-542. 4. Hu Q, et al. J Med Chem. 2010, 53(15), 5749-5758. 5. Bruno RD, et al. Steroids. 2011, 76(12), 1268-1279. 6. Ghoochani A, Hsu E C, Aslan M, et al. Ferroptosis inducers are a novel therapeutic approach for advanced prostate cancer[J]. Cancer research. 2021

文献引用

1. Ghoochani A, Hsu E C, Aslan M, et al. Ferroptosis inducers are a novel therapeutic approach for advanced prostate cancer. Cancer research. 2021 Mar 15;81(6):1583-1594. doi: 10.1158/0008-5472.CAN-20-3477. Epub 2021 Jan 22.
Antihistamine-1 Chalepensin Verapamil hydrochloride Licopyranocoumarin Verapamil TMS Dafadine-A Alizarin

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 抗癌活性化合物库 抗癌药物库 抗癌上市药物库 ReFRAME 相关化合物库 代谢化合物库 抗前列腺癌化合物库 临床期小分子药物库 抑制剂库 已知活性化合物库

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。
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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 154229-19-3 Metabolism P450 Inhibitor Cytochrome P450 CB 7598 inhibit CYPs 阿比特龙 CB7598 CB-7598 inhibitor

 

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