Abiraterone

Catalog No.S1123 Synonyms: CB-7598

Abiraterone Chemical Structure

Molecular Weight(MW): 349.51

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

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2 Customer Reviews

  • A. ZR75-1 (AR+, ER+) and B. MDA MB 231 (AR-, TNBC) cells were treated with either abiraterone or vehicle, then used as targets in a CTL assay using CEA-specific CD8+ T cells as effector cells at an E:T ratio of 30:1. Error bars indicate mean ± S.E.M. for quadruplicate measurements. Statistical analyses were done by Student's t-test, * = P < 0.01 vs. vehicle control. Data are representative of 2 independent experiments.

    Oncotarget, 2016, 7(17):23498-511. Abiraterone purchased from Selleck.

    Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.

    Prostate 2013 74, 235-49. Abiraterone purchased from Selleck.

Purity & Quality Control

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Biological Activity

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.
Targets
CYP17 [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
hamster V79MZh11B1 cells MkS5SpVv[3Srb36gZZN{[Xl? NVPxbJFuUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcDFzQkGgZ4VtdHNuIFnDOVA:OS54MEig{txO NYHZfplkOTh4N{K4Olg>
PC3 cells MkDFR5l1d3SxeHnjxsBie3OjeR?= MXq0PEBp NHG3bItEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjN{IN88US=> M{f0c|I1OTR6OEO3

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[3]
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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 Research:[2]
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  • 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.
    (Only for Reference)
Animal Research:[5]
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  • Animal Models: LAPC-4 xenograft mice
  • Formulation: 0.3% hydroxypropyl cellulose
  • Dosages: 0.15 mmol/kg
  • Administration: Administered via s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMF 4 mg/mL warmed (11.44 mM)
Ethanol 0.2 mg/mL (0.57 mM)
DMSO 0.1 mg/mL (0.28 mM)

* 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 Information

Molecular Weight 349.51
Formula

C24H31NO

CAS No. 154229-19-3
Storage powder
Synonyms CB-7598

Bio Calculators

Molarity Calculator

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Dilution Calculator

Dilution Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01553188 Active, not recruiting Prostatic Neoplams|Prostate Cancer|Neoplasm, Prostate|Neoplasm,Prostatic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 7, 2012 Phase 2
NCT02403505 Not yet recruiting Stage, Prostate Cancer|Surgery Dr. Han Xu, President/CEO / PD / PI / Monitor / IRB Chair|PPD|Medicine Invention Design, Inc August 2020 Phase 3
NCT02949284 Not yet recruiting Stage II Prostate Adenocarcinoma|Stage III Prostate Adenocarcinoma Rutgers, The State University of New Jersey|National Cancer Institute (NCI) June 2017 Phase 2
NCT02987543 Recruiting Metastatic Castration-resistant Prostate Cancer AstraZeneca February 2017 Phase 3
NCT02789878 Not yet recruiting Prostate Cancer Instituto do Cancer do Estado de São Paulo|Janssen, LP February 2017 Phase 2
NCT02867020 Not yet recruiting Prostate Cancer Latin American Cooperative Oncology Group|Janssen Pharmaceuticals January 2017 Phase 2

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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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID