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Formula | C26H33NO2 |
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Molecular Weight | 391.55 | CAS No. | 154229-18-2 | ||||
Solubility (25°C)* | In vitro | DMSO | 11 mg/mL (28.09 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. Abiraterone acetate is an oral androgen biosynthesis inhibitor. | ||
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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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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]. |
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Features | Abiraterone is a drug used in castration-resistant prostate cancer. |
Kinase Assay: |
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Data from [Data independently produced by Endocrinology, 2014, 155(2), 358-69]
Data from [Data independently produced by Prostate, 2013, 74, 235-49]
Data from [Data independently produced by , , Br J Cancer, 2018, doi:10.1038/s41416-018-0158-y]
The Role of CENPK Splice Variant in Abiraterone Response in Metastatic Castration-Resistant Prostate Cancer [ Cells, 2024, 13(19)1622] | PubMed: 39404386 |
Plk1 Inhibitors and Abiraterone Synergistically Disrupt Mitosis and Kill Cancer Cells of Disparate Origin Independently of Androgen Receptor Signaling [ Cancer Res, 2023, 83(2):219-238] | PubMed: 36413141 |
Androgen receptor blockade resistance with enzalutamide in prostate cancer results in immunosuppressive alterations in the tumor immune microenvironment [ J Immunother Cancer, 2023, 11(5)e006581] | PubMed: 37147019 |
Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models [ Pharmacol Res, 2023, 189:106692] | PubMed: 36773708 |
Novel inhibition of AKR1C3 and androgen receptor axis by PTUPB synergizes enzalutamide treatment in advanced prostate cancer [ Oncogene, 2023, 42(9):693-707] | PubMed: 36596844 |
Novel inhibition of AKR1C3 and androgen receptor axis by PTUPB synergizes enzalutamide treatment in advanced prostate cancer [ Oncogene, 2023, 42(9):693-707] | PubMed: 36596844 |
Loss of Long Noncoding RNA NXTAR in Prostate Cancer Augments Androgen Receptor Expression and Enzalutamide Resistance [ Cancer Res, 2022, 82(1):155-168] | PubMed: 34740892 |
miR-143 mediates abiraterone acetate resistance by regulating the JNK/Bcl-2 signaling pathway in prostate cancer [ J Cancer, 2022, 13(15):3652-3659] | PubMed: 36606191 |
Abiraterone acetate induces CREB1 phosphorylation and enhances the function of the CBP-p300 complex, leading to resistance in prostate cancer cells [ Clin Cancer Res, 2021, clincanres.4391.2020] | PubMed: 33495313 |
Antiproliferative, proapoptotic, and tumor-suppressing effects of the novel anticancer agent alsevirone in prostate cancer cells and xenografts [ Arch Pharm (Weinheim), 2021, e2100316] | PubMed: 34668210 |
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