Abiraterone

Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.

Product Specifications

CAS Number

[154229-19-3]

Product Name Alternative

CB-7598

UNSPSC

12352005

Hazard Statement

H360, H373, H410

Target

Cytochrome P450

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Abiraterone.html

Purity

99.92

Solubility

DMF : 5 mg/mL (ultrasonic; warming; heat to 60°C) |DMSO : 2.5 mg/mL (ultrasonic; warming; heat to 60°C) |Ethanol : 5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C[C@@]12C(C3=CN=CC=C3)=CC[C@]1([C@@]4(CC=C5[C@@](C)([C@]4(CC2)[H])CC[C@@H](C5)O)[H])[H]

Molecular Formula

C24H31NO

Molecular Weight

349.51

Precautions

H360, H373, H410

References & Citations

[1]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. J Clin Oncol. 2008 Oct 1;26 (28) :4563-71.|[2]Richards J, et al. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72 (9) :2176-82.|[3]Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16 (3) :387-400.|[4]Li R, et al. Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clin Cancer Res. 2012 Jul 1;18 (13) :3571-9.|[5]Kumar SV, et al. Validated RP-HPLC/UV method for the quantitation of abiraterone in rat plasma and its application to a pharmacokinetic study in rats. Biomed Chromatogr. 2013 Feb;27 (2) :203-7.|[6]Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16 (3) :387-400.