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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 evalsuating 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.

Reference:

• 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.