Abiraterone Acetate

Catalog No.S2246 Synonyms: CB7630

Abiraterone Acetate Chemical Structure

Molecular Weight(MW): 391.55

Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.

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3 Customer Reviews

  • Concomitant Western blot analysis of ER and TFF1 assessed after 16 h treatment with E2 or abiraterone in the presence or absence of MG-132 (10 μM).

    Br J Cancer, 2018, doi:10.1038/s41416-018-0158-y. Abiraterone Acetate purchased from Selleck.

    BCaPT10 and BPH-1 cells were treated with vehicle (NTC, white bars), 10 uM abiraterone (ABI, gray bars), or abiraterone plus steroid hormones (black bars, 100 nM DHT, 10 nM estradiol, and 10 nM progestin). Minimum of 200 cells per condition was used from each of at least 3 independent experiments. Each result is shown as the average 盨EM from at least 3 independent experiments. One-way ANOVA. *, P < .05; **, P < .01; ***, P < .005; ****, P < .001.

    Endocrinology 2014 155(2), 358-69. Abiraterone Acetate 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 Acetate purchased from Selleck.

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Biological Activity

Description Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.
Features Abiraterone is a drug used in castration-resistant prostate cancer.
Targets
CYP17 [1]
(Cell-free assay)
72 nM
In vitro

Abiraterone shows a good complexation with the heme iron only in SM1. [1] Abiraterone blocks the synthesis of androgens by inhibiting CYP17A1. Abiraterone also blocks 3β-hydroxysteroid dehydrogenase (3βHSD), an enzyme that is absolutely required for the synthesis of biologically active androgens. Abiraterone inhibits conversion of DHEA to Δ4-androstenedione. Abiraterone inhibition of 3βHSD blocks DHT synthesis and the androgen receptor response. Abiraterone inhibits the conversion of Δ5-androstenediol to testosterone. [2] Abiraterone inhibits C17,20-lyase, with an IC50 of 5.8 nM, in rat testis microsomes. Abiraterone significantly inhibits testosterone secretion (−48%) and in turn increases LH concentration (192%). [3] Abiraterone inhibits in vitro proliferation and AR-regulated gene expression of AR-positive prostate cancer cells, which could be explained by AR antagonism in addition to inhibition of steroidogenesis. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
hamster V79MZh11B1 cells MYPGeY5kfGmxbjDhd5NigQ>? M3;tfmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJzIHPlcIx{NCCLQ{WwQVEvPjB6IN88US=> M{nwTVE5Pjd{OE[4
V79MZh11B1 cells NFmyVWVHfW6ldHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IFPZVFEySjFiZYjwdoV{e2WmIHnuJIV5eHKnc4Pl[EBqdiCYN{nNXogyOUJzIHPlcIx{NCCLQ{WwQVEvPjB6IN88US=> NFPsfGQyQTJzMUG3OC=>
hamster V79MZh cells NIXieZZHfW6ldHnvckBie3OjeR?= MojRTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczygTWM2OD1zLk[xJO69VQ>? MWiyNFU2ODFzOB?=
human PC3 cells MmriR5l1d3SxeHnjxsBie3OjeR?= M4DGeFQ5KGh? NEf0NVlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjN{IN88US=> MkLHNlQyPDh6M{e=

... Click to View More Cell Line Experimental Data

In vivo Following intraperitoneal administration in a rodent model, abiraterone was found to have rapid deacetylation. When administered as its acetate pro-drug (CB 7630), it suppressed circulating testosterone to undetectable levels and markedly decreased the weights of androgen sensitive organs. Abiraterone is well tolerated and the mean elimination half-life of abiraterone in these studies was 27.6 h (thus supporting the use of once-daily dosing)[5]. Preclinical studies with abiraterone demonstrated reduction in androgen production downstream of CYP17 which resulted in decreased weight of the ventral prostate, testis, and seminal vesicles in mice[6].

Protocol

Kinase Assay:

[3]

+ Expand

C17,20-lyase activity assay:

Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contains 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, test compounds are 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 in our laboratory using a specific antibody against Δ4A and instructions provided by Biogenesis. 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 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:

[4]

+ Expand
  • Cell lines: LNCaP and VCaP cells
  • Concentrations: 0 μM -10 μM
  • Incubation Time: 24 hours and 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:

[2]

+ Expand
  • Animal Models: Male NOD/SCID mice with LAPC4 cells
  • Formulation: 0.1 mL 5% benzyl alcohol and 95% safflower oil solution
  • Dosages: 0.5 mmol/kg/d
  • Administration: Administered via s.c.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 28 mg/mL (71.51 mM)
DMSO Insoluble
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+95% Corn oil
For best results, use promptly after mixing.
30 mg/mL

* 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 391.55
Formula

C26H33NO2

CAS No. 154229-18-2
Storage powder
in solvent
Synonyms CB7630

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02849990 Recruiting Stage III Prostate Adenocarcinoma AJCC v7|Stage III Prostate Cancer AJCC v7|Stage IV Prostate Adenocarcinoma AJCC v7|Stage IV Prostate Cancer AJCC v7 University of Washington|Janssen Scientific Affairs LLC|National Cancer Institute (NCI) March 9 2017 Phase 2
NCT02485691 Recruiting Prostate Cancer Metastatic Sanofi November 9 2015 Phase 4
NCT02123758 Active not recruiting Prostatic Neoplasms|Metastatic Castration-Resistant Prostate Cancer Aragon Pharmaceuticals Inc. July 9 2014 Phase 1
NCT01695135 Completed Prostate Neoplasms Janssen Research & Development LLC August 9 2012 Phase 3
NCT01650194 Completed Metastatic Castration-Resistant Prostate Cancer Astellas Pharma Global Development Inc.|Medivation Inc.|Astellas Pharma Inc July 9 2012 Phase 2
NCT01309672 Active not recruiting Prostate Cancer Southwest Oncology Group|National Cancer Institute (NCI) August 9 2011 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID