Home Metabolism P450 (e.g. CYP17) inhibitor - Androgen Receptor inhibitor Abiraterone For research use only.

Abiraterone

Synonyms: CB-7598

Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.

Abiraterone Chemical Structure

Abiraterone Chemical Structure

CAS: 154229-19-3

Selleck's Abiraterone has been cited by 34 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
JM109 Growth inhibition assay Inhibition of C-terminal His-tagged recombinant human CYP17A1delta19H mutant expressed in Escherichia coli JM109 cells assessed as decrease in progesterone hydroxylation in presence of cytochrome P450 reductase by HPLC-UV method, IC50=0.0094μM. 29792703
P450c17-LNCaP Growth inhibition assay In vitro cytochrome P450 17A1 inhibition was assayed using the rapid acetic acid releasing assay (AARA), utilizing intact P450c17-expressing Escherichia coli or P450c17-LNCaP cells as the enzyme source, IC50=0.8μM. 12773039
V79MZh11B1 Growth inhibition assay Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=1.608μM. 18672868
V79MZh11B1 Growth inhibition assay Inhibition of recombinant CYP11B1 expressed in expressed in V79MZh11B1 cells, IC50=1.608μM. 19211174
V79MZh Growth inhibition assay Inhibition of human CYP11B1 expressed in hamster V79MZh cells, IC50=1.61μM. 20550118
V79MZh Growth inhibition assay Inhibition of human CYP11B1 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate, IC50=1.61μM. 23859149
V79MZh Growth inhibition assay Inhibition of human CYP11B2 expressed in hamster V79MZh cells, IC50=1.75μM. 20550118
V79MZh Growth inhibition assay Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate, IC50=1.75μM. 23859149
V79MZh11B2 Growth inhibition assay Inhibition of human CYP11B2 expressed in hamster V79MZh11B2 cells, IC50=1.751μM. 18672868
LNCAP Antiproliferative assay 72 hrs Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay, IC50=3.29μM. 29310026
hTERT-BJ Cytotoxicity assay 48 hrs Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay, GI50=4.5μM. 29172080
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50=5.94μM. 29310026
MGC803 Antiproliferative assay 72 hrs Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay, IC50=7.72μM. 29310026
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50=7.9μM. 29172080
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=9.32μM. 24148837
GES-1 Antiproliferative assay 72 hrs Antiproliferative activity against human GES-1 cells after 72 hrs by MTT assay, IC50=13.12μM. 29310026
T47D Growth inhibition assay 72 hrs Growth inhibition of human T47D cells after 72 hrs by MTT assay, IC50=16.9μM. 27209562
MDA-MB-231 Growth inhibition assay 72 hrs Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=19.2μM. 27209562
MCF7 Growth inhibition assay 72 hrs Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50=19.3μM. 27209562
MDA-MB-361 Growth inhibition assay 72 hrs Growth inhibition of human MDA-MB-361 cells after 72 hrs by MTT assay, IC50=20.4μM. 27209562
T47D Antiproliferative assay 48 hrs Antiproliferative activity against human T47D cells after 48 hrs by SRB assay, GI50=24μM. 29172080
WiDr Antiproliferative assay 48 hrs Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay, GI50=42μM. 29172080
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Biological Activity

Description Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.
Features Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.
Targets
CYP17 [1]
(Cell-free assay)
2 nM
In vitro
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot eIF4E / eIF4G / eIF4E / eIF4G / AR p-4EBP1 / 4EBP1 22174412
In Vivo
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]
Animal Research Animal Models LAPC-4 xenograft mice
Dosages 0.15 mmol/kg
Administration Administered via s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06014853 Recruiting Prostate Cancer Bukwang Pharmaceutical|Dyna Therapeutics August 7 2023 Phase 1
NCT03348670 Active not recruiting Prostate Cancer Han Xu M.D. Ph.D. FAPCR Sponsor-Investigator IRB Chair|Medicine Invention Design Inc August 18 2023 Phase 2|Phase 3
NCT05737082 Completed Healthy Hanmi Pharmaceutical Company Limited March 10 2023 Phase 1

Chemical lnformation & Solubility

Molecular Weight 349.51 Formula

C24H31NO
CAS No. 154229-19-3 SDF Download Abiraterone SDF
Smiles CC12CCC(CC1=CCC3C2CCC4(C3CC=C4C5=CN=CC=C5)C)O
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 0.2 mg/mL

DMSO : 0.1 mg/mL ( (0.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 0.02 mg/mL


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