Abiraterone(CB-7598)/阿比特龙 CYP17YZ剂

Abiraterone(CB-7598)/阿比特龙
Molecula Formula:C24H31NO
Molecular Weight: 349.51
Appearance: White or off-white powder
Purity:99%
CAS[154229-19-3]

Biological Activity:
Abiraterone (CB-7598) is a potent steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor with an IC50 at 4 nM.
Abiraterone (CB-7598) is currently undergoing phase II clinical trials as a potential compound for the treatment of prostate cancer. In preclinical studies, abiraterone (CB-7598) has demonstrated the ability to selectively inhibit the target enzyme, resulting in inhibition of testosterone production in both the adrenals and the testes. Clinical studies demonstrated that CYP17 blockade by abiraterone acetate is safe and has significant antitumor activity in CRPC (castration-resistant prostate cancer).

References:
[1]. Pinto-Bazurco Mendieta, Mariano A. E.; Synthesis, Biological Evaluation, and Molecular Modeling of Abiraterone Analogues: Novel CYP17 Inhibitors for the Treatment of Prostate Cancer. Journal of Medicinal Chemistry (2008), 51(16), 5009-5018.
[2]. Attard G et al Selective inhibition of CYP17 with abiraterone acetate is highly active in the treatment of castration-resistant prostate cancer. J Clin Oncol. 2009 Aug 10;27(23):3742-8.