Abiraterone

Catalog No.S1123

Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.

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Abiraterone Chemical Structure

Abiraterone Chemical Structure
Molecular Weight: 349.51

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Related Compound Libraries

Abiraterone is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.
Targets CYP17 [1]
(Cell-free assay)
IC50 2 nM
In vitro 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. [2]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%).[3]
In vivo Abiraterone inhibits CYP17 with an IC50 of 72 nM, in human testicular microsomes. [4] Abiraterone fails to significantly reduce the size of any of the organs. [5] 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. [6]
Features Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.

Protocol(Only for Reference)

Kinase Assay: [3]

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.

Cell Assay: [2]

Cell lines LNCaP and VCaP cells
Concentrations 0.1-5 μM
Incubation Time 24 hours or 96 hours
Method LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence.

Animal Study: [5]

Animal Models LAPC-4 xenograft mice
Formulation 0.3% hydroxypropyl cellulose
Dosages 0.15 mmol/kg
Administration Administered via s.c.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Attard G, et al. J Clin Oncol. 2008, 26(28), 4563-4571.

[2] Richards J, et al. Cancer Res. 2012, 72(9), 2176-2182.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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  ...more 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

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Chemical Information

Download Abiraterone SDF
Molecular Weight (MW) 349.51
Formula

C24H31NO

CAS No. 154229-19-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CB-7598
Solubility (25°C) * In vitro DMF 4 mg/mL warming (11.44 mM)
Ethanol 0.2 mg/mL (0.57 mM)
DMSO 0.1 mg/mL (0.28 mM)
In vivo
* <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.
Chemical Name 17-​(3-​pyridinyl)​-​(3β)​-androsta-​5,​16-​dien-​3-​ol

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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