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Abiraterone Acetate (CB7630)
Catalog No.S2246 Synonyms: CB7630, CB-7630
For research use only.
Abiraterone Acetate (CB7630, CB-7630) 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 27 publications
Purity & Quality Control
Choose Selective P450 (e.g. CYP17) Inhibitors
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Biological Activity
| Description | Abiraterone Acetate (CB7630, CB-7630) 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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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)
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Solubility (25°C)
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In vitro |
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In vivo |
Add solvents to the product individually and in order |
0.5mg/ml |
Chemical Information
| Molecular Weight | 391.55 | ||
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| 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 | ||
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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
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04587427 | Active not recruiting | Drug: Radium 223 dichloride (Xofigo BAY88-8223) | Bone Metastatic Castration-resistant Prostate Cancer | Bayer | March 31 2022 | -- |
| NCT05376722 | Active not recruiting | Drug: pamiparib|Drug: abiraterone|Drug: prednisone | Neoadjuvant Therapy | Hongqian Guo|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School | February 22 2022 | Phase 2 |
| NCT05177042 | Recruiting | Drug: ARV-110 in Combination with Abiraterone | Prostate Cancer Metastatic | Arvinas Androgen Receptor Inc.|Arvinas Inc. | February 1 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 |
(data from https://clinicaltrials.gov, updated on 2022-08-01)
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