Abiraterone

• Description:

  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 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  CYP17

• CAS Number:

  154229-19-3