|Solubility:||DMSO up to 20mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
Abiraterone is the first-in-class potent and selective CYP17 (cytochrome P450 17alpha-hydroxylase-17,20-lyase) inhibitor with IC50 ~4 nM. It was approved by US FDA in 2011 to treat castration-resistant prostate cancer. As prostate cancer cells proliferate in response to androgen steroids, CYP17 inhibition is a new strategy to prevent androgen synthesis and treat lethal metastatic prostate cancer. In recent Nature publication, the structures of cytochrome P450 17A1 with abiraterone was released. A phase I/II clinical trial evaluating abiraterone in advanced breast cancer patients is also underway.
How to Use:
In vitro: Abiraterone is typically used at 1 ¦ÌM concentration in vitro.
In vivo: Abiraterone acetate (pro-drug) was dosed to mice and rats at 50 mg/kg orally once per day.
- 1. Jarman M, et al. The 16,17-double bond is needed for irreversible inhibition of human cytochrome p45017alpha by abiraterone (17-(3-pyridyl)androsta-5, 16-dien-3beta-ol) and related steroidal inhibitors. (1998) J Med Chem. 41(27):5375-81.
- 2. Attard G et al. Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that castration-resistant prostate cancer commonly remains hormone driven. (2008) J Clin Oncol. 26(28):4563-71.
- 3. Attard G et al. Selective inhibition of CYP17 with abiraterone acetate is highly active in the treatment of castration-resistant prostate cancer. (2009) J Clin Oncol. 27(23):3742-8.
- 4. de Bono JS, et al. Abiraterone and increased survival in metastatic prostate cancer. (2011) N Engl J Med. 364(21):1995-2005.
- 5. DeVore NM, et al. Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001. (2012) Nature. 482(7383):116-9.
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