Abiraterone acetate
(Synonyms: 乙酸阿比特龙酯,CB7630) 目录号 : GC11108
A CYP17A1 inhibitor
Cas No.:154229-18-2
Sample solution is provided at 25 µL, 10mM.
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Abiraterone acetate is the 3β-acetate form of its active component abiraterone, a potent inhibitor of androgen biosynthesis. Abiraterone, a pregnenolone-derived 3-pyridyl steroidal compound, potently and irreversibly inhibits cytochrome P450 17 alpha-hydroxylase (CYP17), an important enzyme involved in the synthesis of androgen and cortisol, through a covalent binding mechanism with a value of 50% inhibition concentration IC50 of 72 nM, which is 10 to 30 times greater in potency, due to the 3-pyridyl substitution in its chemical structure, than the inhibition by ketoconazole. In order to improve the low solubility of abirateone, abiraterone acetate has been developed and used for the treatment of castration-resistant prostate cancer (CRPC).
Reference
[1].Charles J Ryan and Michael L Cheng. Abiraterone acetate for the treatment of prostate cancer. Expert Opin. Pharmacother. (2013) 14 (1): 91-96
[2].Tadas S. Vasaitis, Robert D. Bruno and Vincent C.O. Njar. CYP17 inhibitors for prostate cancer therapy. Journal of Steroid Biochemistry & Molecular Biology 125 (2011) 23-31
[3].Guru Sonpavde, Gerhardt Attard, Joaquim Bellmunt, Malcolm D. Mason, Bernard Malavaud, Bertrand Tombal and Cora N. Sternberg. The role of abiraterone acetate in the management of prostate cancer: a critical analysis of the literature. EUROPEAN UROLOGY 60 (2011) 270-278
| Cell experiment [1]: | |
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Cell lines |
PC-3 cells |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.1 ~ 25 μM; 16 hrs |
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Applications |
In PC-3 cells co-transfected with ARE3-luciferase and wild type or mutant androgen receptor (AR), Abiraterone Acetate at the dose up to 25 μM did not any obvious increase in luciferase activity. However, Abiraterone Acetate dose-dependently inhibited stimulated wild type and mutant AR activity, with significant inhibition observed at the doses ≤ 10 μM. |
| Animal experiment [2]: | |
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Animal models |
Male NOD/SCID mice bearing LAPC4 cells |
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Dosage form |
0.5 mmol/kg/d; i.p.; 5 days per week, for 4 weeks |
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Applications |
Abiraterone Acetate at the dose of 0.5 mmol/kg/d resulted in serum concentrations ranging from 0.5 to 1 mmol/L. Compared with the control group, Abiraterone Acetate treatment significantly inhibited "castration-resistant" prostate cancer progression in the robustly growing subset, effectively inhibiting tumor growth over 4 weeks of treatment. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Richards J, Lim AC, Hay CW, Taylor AE, Wingate A, Nowakowska K, Pezaro C, Carreira S, Goodall J, Arlt W, McEwan IJ, de Bono JS, Attard G. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82. [2]. Li R, Evaul K, Sharma KK, Chang KH, Yoshimoto J, Liu J, Auchus RJ, Sharifi N. Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clin Cancer Res. 2012 Jul 1;18(13):3571-9. | |
| Cas No. | 154229-18-2 | SDF | |
| 别名 | 乙酸阿比特龙酯,CB7630 | ||
| 化学名 | [(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-pyridin-3-yl-2,3,4,7,8,9,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-3-yl] acetate | ||
| Canonical SMILES | CC(=O)OC1CCC2(C3CCC4(C(C3CC=C2C1)CC=C4C5=CN=CC=C5)C)C | ||
| 分子式 | C26H33NO2 | 分子量 | 391.55 |
| 溶解度 | ≥ 15.7mg/mL in Ethanol, ≥ 11.22 mg/mL in DMSO with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.554 mL | 12.7698 mL | 25.5395 mL |
| 5 mM | 0.5108 mL | 2.554 mL | 5.1079 mL |
| 10 mM | 0.2554 mL | 1.277 mL | 2.554 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet