Catalog No.S1123 Synonyms: CB-7598
Molecular Weight(MW): 349.51
Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.
Cited by 7 Publications
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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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|Description||Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.|
|Features||Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.|
Abiraterone binds and inhibits wild-type and mutant androgen receptor (AR). Abiraterone inhibits in vitro proliferation and androgen receptor-regulated gene expression of androgen receptor-positive prostate cancer cells, which could be explained by androgen receptor antagonism in addition to inhibition of steroidogenesis. In fact, activation of mutant androgen receptor by eplerenone is inhibited by greater concentrations of Abiraterone. Abiraterone displaces ligand from both WT-AR and T877A with EC50 of 13.4 μM and 7.9 μM, respectively. Abiraterone inhibits lyase activity with an IC50 of 5.8 nM in rat testis microsomes. Abiraterone acetate significantly inhibits T secretion (−48%) and in turn increased LH concentration (192%).
|In vivo||Abiraterone inhibits CYP17 with an IC50 of 72 nM, in human testicular microsomes.  Abiraterone fails to significantly reduce the size of any of the organs.  Abiraterone reduces the testosterone levels strongly, almost reaching the level of the orchiectomy control. The testosterone levels are reduced by Abiraterone for more than 95% compared to the control group. |
C17,20-lyase activity assay:Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contained 0.25 M sucrose, 20 mM Tris–HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, Abiraterone is evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at −20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format using a specific antibody against Δ4A. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a 1450 MicrobetaPlus liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration.
-  Attard G, et al. J Clin Oncol. 2008, 26(28), 4563-4571.
-  Richards J, et al. Cancer Res. 2012, 72(9), 2176-2182.
-  Duc I, et al. J Steroid Biochem Mol Biol. 2003, 84(5), 537-542.
|In vitro||DMF||4 mg/mL (11.44 mM) warming|
|Ethanol||0.2 mg/mL (0.57 mM)|
|DMSO||0.1 mg/mL (0.28 mM)|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02789878||Not yet recruiting||Prostate Cancer||Instituto do Cancer do Estado de São Paulo|Janssen, LP||November 2016||Phase 2|
|NCT02807805||Not yet recruiting||Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer||University of California, Davis|National Cancer Institute (NCI)||October 2016||Phase 2|
|NCT02543255||Not yet recruiting||Castration-resistant Prostate Cancer||University Health Network, Toronto||October 2016||Phase 2|
|NCT02849990||Not yet recruiting||Stage III Prostate Adenocarcinoma|Stage III Prostate Cancer|Stage IV Prostate Adenocarcinoma|Stage IV Prostate Cancer||University of Washington|National Cancer Institute (NCI)||August 2016||Phase 2|
|NCT02608359||Recruiting||Prostate Cancer||Johnson & Johnson Private Limited||May 2016||Phase 4|
|NCT02703623||Recruiting||Prostate Cancer||M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi||May 2016||Phase 2|
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