| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 50mg | 电议 |
Cell lines | PC-3 cells |
Preparation method | The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months. |
Reacting condition | 0.1 ~ 25 μM; 16 hrs |
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 models | Male NOD/SCID mice bearing LAPC4 cells |
Dosage form | 0.5 mmol/kg/d; i.p.; 5 days per week, for 4 weeks |
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. |
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. |
| 产品描述 | 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 IC50of 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 |
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