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Abiraterone Acetate (CB7630)
Catalog No.S2246
For research use only.
Abiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor.
CAS No. 154229-18-2
Selleck's Abiraterone Acetate (CB7630) has been cited by 26 publications
Purity & Quality Control
Choose Selective P450 (e.g. CYP17) Inhibitors
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Other P450 (e.g. CYP17) Products
Biological Activity
| Description | Abiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Features | Abiraterone is a drug used in castration-resistant prostate cancer. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Targets |
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| 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] |
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| Cell Data |
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| 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 (from reference)
| Kinase Assay: |
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| Cell Research: |
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| Animal Research: |
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Solubility (25°C)
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In vitro |
DMSO |
Insoluble
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| Water |
Insoluble
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| Ethanol |
''''28 mg/mL
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In vivo |
Add solvents to the product individually and in order |
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 |
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| CAS No. | 154229-18-2 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC(=O)OC1CCC2(C3CCC4(C(C3CC=C2C1)CC=C4C5=CN=CC=C5)C)C | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04587427 | Not yet recruiting | Drug: Radium 223 dichloride (Xofigo BAY88-8223) | Metastatic Castration-resistant Prostate Cancer (mCRPC) | Bayer | March 31 2022 | -- |
| NCT05177042 | Recruiting | Drug: ARV-110 in Combination with Abiraterone | Prostate Cancer Metastatic | Arvinas Androgen Receptor Inc.|Arvinas Inc. | January 7 2022 | Phase 1 |
| NCT04887506 | Recruiting | Drug: TAVT-45|Drug: Zytiga|Drug: Prednisone | Metastatic Castration-resistant Prostate Cancer|Metastatic Castration-sensitive Prostate Cancer|Metastatic Prostate Cancer | Tavanta Therapeutics | April 14 2021 | Phase 3 |
| NCT04862091 | Recruiting | Drug: Abiraterone Acetate Tablets (I)|Drug: ZYTIGA® | Metastatic Castration-resistant Prostate Cancer (mCRPC) | Jiangsu HengRui Medicine Co. Ltd. | April 23 2021 | Phase 2 |
| NCT04458311 | Recruiting | Drug: Abiraterone Acetate|Drug: Tildrakizumab | Metastatic Castration Resistant Prostate Cancer | Institute of Cancer Research United Kingdom|Sun Pharmaceutical Industries Limited | December 1 2020 | Phase 1|Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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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