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.
CAS Number: 154229-19-3
Molecular Weight: 349.51
Chemical Name: (3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 20mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Abiraterone is typically used at 1 μM concentration in vitro.
Abiraterone acetate (pro-drug) was dosed to mice and rats at 50 mg/kg orally once per day.
- 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.
- 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.
- DeVore NM, et al. Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001. (2012) Nature. 482(7383):116-9.
Products are for research use only. Not for human use.
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