Biological Activity:
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 μM concentration in vitro.
In vivo:?Abiraterone acetate (pro-drug) was dosed to mice and rats at 50 mg/kg orally once per day.
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Reference:
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