Abiraterone acetate
Based on 24 publication(s) in Google Scholar
Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 154229-18-2
- Formula: C26H33NO2
- Molecular Weight:391.55
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Abiraterone acetate
More- Cell Rep Med. 2024 Feb 20;5(2):101388. [Abstract]
- Cell Death Dis. 2022 Dec 12;13(12):1034. [Abstract]
- Cell Death Dis. 2021 Aug 12;12(8):787. [Abstract]
- Br J Pharmacol. 2025 Dec 17. [Abstract]
- Br J Cancer. 2017 Mar 28;116(7):937-943. [Abstract]
- JCI Insight. 2019 Sep 5;4(17):e122688. [Abstract]
- Mol Cancer Ther. 2015 Jan;14(1):59-69. [Abstract]
- J Enzyme Inhib Med Chem. 2025 Dec;40(1):2463014. [Abstract]
- Cells. 2022 Jan 18;11(3):319. [Abstract]
- Int J Mol Sci. 2023 Jan 30;24(3):2579. [Abstract]
- Biomolecules. 2024 Feb 8;14(2):203. [Abstract]
- Biomolecules. 2023 Sep 5;13(9):1349. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- J Neuroendocrinol. 2022 Mar 24;e13128. [Abstract]
- Biomedicines. 2026 May;14(5):949.
- Prostate. 2025 Sep 19. [Abstract]
- Preprints. 2025 Dec 3.
- Patent. US20250268958A1.
- SSRN. 2024 Dec 30.
- bioRxiv. 2024 October 25.
- bioRxiv. 2023 Nov 2.
- Preprints. 2023 Nov 1.
- University of Valencia. 2020 Jul.
- Psychology, University of British Columbia. 2017 Aug.
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ELISA
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WB
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RT-PCR
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
Biological Activity
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CYP17 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16 | IC50 |
28.74 μM
Compound: 4a
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Antiproliferative activity against mouse B16 cells measured after 48 hrs by MTT assay
Antiproliferative activity against mouse B16 cells measured after 48 hrs by MTT assay
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[PMID: 38467086] |
| PC-3 | IC50 |
37.61 μM
Compound: Abiraterone
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Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35244394] |
| SK-OV-3 | IC50 |
51.51 μM
Compound: Abiraterone
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Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35244394] |
| T47D | IC50 |
34.66 μM
Compound: Abiraterone
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Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35244394] |
Abiraterone (Abi) acetate is an ester prodrug of the anticancer agent Abiraterone, which shows IC50 values of 15 nM and 2.5 nM for the 17,20-lyase and 17α-hydroxylase (CYP17 is a bifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activity). Abiraterone inhibits human 17,20-lyase and 17α-hydroxylase with IC50 of 27 and 30 nM respectively[1]. Significant inhibition of proliferation of the AR-positive prostate cancer cell lines LNCaP and VCaP with doses of Abiraterone ≥5 μM is confirmed[2]. Abiraterone inhibits recombinant human 3βHSD1 and 3βHSD2 activity with competitive Ki values of 2.1 and 8.8 μM. 10 μM Abiraterone is sufficient to completely block synthesis of 5α-dione and DHT in both cell lines.Treatment with Abiraterone significantly inhibited CRPC progression in the robustly growing subset, effectively putting a ceiling on tumor growth over 4 weeks of treatment (P<0.00001)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 154229-18-2
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Appearance Solid
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Molecular Weight 391.55
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Formula C26H33NO2
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Color White to off-white
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SMILES
O=C(O[C@@H]1CC2=CC[C@]3([H])[C@]([H])(CC[C@](C)(C(C4=CN=CC=C4)=CC5)[C@]35[H])[C@@]2(C)CC1)C
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Synonyms
CB7630
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (24)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer. [Abstract]2024 Feb 20;5(2):101388. PMID: 38262412
Abiraterone acetate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Feb 20;5(2):101388. [Abstract]
Abiraterone acetate (ABI) (10 µM; 48 h) induced ACh secretion in 22Rv1 cells.
Abiraterone acetate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Feb 20;5(2):101388. [Abstract]
Abiraterone acetate (ABI) (10 µM; 48 h) induced CHRM1 protein expression in 22Rv1 cells.
Abiraterone acetate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Feb 20;5(2):101388. [Abstract]
Abiraterone acetate (ABI) (10 µM; 24-48 h) increased CHAT, VACHT, and ACHE mRNA levels in 22Rv1 cells.
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Cell Death Dis
Idarubicin combats abiraterone and enzalutamide resistance in prostate cells via targeting XPA protein. [Abstract]2022 Dec 12;13(12):1034. PMID: 36509750
Abiraterone acetate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Dec 12;13(12):1034. [Abstract]
LNCaP-derived xenografts of castrated male null mice were sensitive to Abiraterone acetate (ABI; AA) (0.5 mmol/kg, i.g.) treatment.
Abiraterone acetate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Dec 12;13(12):1034. [Abstract]
Abiraterone acetate (ABI; AA) (0.5 mM/kg) caused the curve of the cumulative frequency of sgRNAs to shift toward the left in LNCaP/ABI-derived xenograft mice.
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Cell Death Dis
KAT2A-mediated AR translocation into nucleus promotes abiraterone-resistance in castration-resistant prostate cancer. [Abstract]2021 Aug 12;12(8):787. PMID: 34381019 -
Br J Pharmacol
Anti-mitotic agent SB-216 overcomes taxane resistance in castration-resistant prostate cancer and exhibits anti-tumour efficacy in pancreatic cancer. [Abstract]2025 Dec 17. PMID: 41408705 -
Br J Cancer
2017 Mar 28;116(7):937-943. PMID: 28253524
Abiraterone acetate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2017 Mar 28;116(7):937-943. [Abstract]
Targeting the androgen signaling axis decreases tumour growth in AR-positive human RCC cell line, Caki2, xenografts. (A) After inoculating the flanks with Caki2, 30 mice are randomized into six groups of five mice each. The treatment is rendered as indicated. Both enzalutamide (Enz) and Abiraterone acetate (AA) decrease tumor volume dramatically. (B) Gross picture of tumors collected from mice after treatment. (C) After establishing the tumors, 30 mice are surgically castrated and treated with t
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JCI Insight
Targeting castration-resistant prostate cancer with androgen receptor antisense oligonucleotide therapy. [Abstract]2019 Sep 5;4(17):e122688. PMID: 31484823 -
Mol Cancer Ther
Anticancer activity of a novel selective CYP17A1 inhibitor in preclinical models of castrate-resistant prostate cancer. [Abstract]2015 Jan;14(1):59-69. PMID: 25351916 -
J Enzyme Inhib Med Chem
2025 Dec;40(1):2463014. PMID: 39950830 -
Cells
Assessment of FDA-Approved Drugs as a Therapeutic Approach for Niemann-Pick Disease Type C1 Using Patient-Specific iPSC-Based Model Systems. [Abstract]2022 Jan 18;11(3):319. PMID: 35159129 -
Int J Mol Sci
2023 Jan 30;24(3):2579. PMID: 36768902 -
Biomolecules
2024 Feb 8;14(2):203. PMID: 38397440 -
Biomolecules
2023 Sep 5;13(9):1349. PMID: 37759751 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
J Neuroendocrinol
Androgen synthesis inhibition increases behavioural flexibility and mPFC tyrosine hydroxylase in gonadectomized male rats. [Abstract]2022 Mar 24;e13128. PMID: 35583989 -
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Prostate
MIF Facilitates Resistance to Androgen Deprivation Therapy by Regulating AMPD2 Expression in Prostate Cancer Cells. [Abstract]2025 Sep 19. PMID: 40968720 -
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Solvent & Solubility
DMSO : 10 mg/mL (25.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.55 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.55 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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 (5 μM and 10 μM) at 24 and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Male NOD/SCID mice 6 to 8 weeks of age are surgically orchiectomized and implanted with a 5 mg 90-day sustained release DHEA pellet to mimic CRPC with human adrenal physiology. Two days later, 7×106 LAPC4 cells are injected subcutaneously with Matrigel. Tumor dimensions are measured 2 to 3 times per week, and volume is calculated as length×width×height×0.52. Once tumors reach 300 mm3, mice are randomly assigned to vehicle or Abiraterone treatment groups. Mice in the Abiraterone group are treated with 5 mL/kg intraperitoneal injections of 0.5 mmol/kg/d (0.1 mL 5% benzyl alcohol and 95% safflower oil solution) and control mice with vehicle only, once daily for 5 days per week over a duration of 4 weeks (n=8 mice per treatment). Statistical significance between Abiraterone and vehicle treatment groups is assessed by ANOVA based on a mixed-effect model.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16(3):387-400. [Content Brief]
[2]. Richards J, et al. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82. [Content Brief]
[3]. Li R, et al. Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clin Cancer Res. 2012 Jul 1;18(13):3571-9. [Content Brief]
[4]. Lee GT, et al. Intracrine androgen biosynthesis in renal cell carcinoma. Br J Cancer. 2017 Mar 28;116(7):937-943. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5540 mL | 12.7698 mL | 25.5395 mL | 63.8488 mL |
| 5 mM | 0.5108 mL | 2.5540 mL | 5.1079 mL | 12.7698 mL | |
| 10 mM | 0.2554 mL | 1.2770 mL | 2.5540 mL | 6.3849 mL | |
| 15 mM | 0.1703 mL | 0.8513 mL | 1.7026 mL | 4.2566 mL | |
| 20 mM | 0.1277 mL | 0.6385 mL | 1.2770 mL | 3.1924 mL | |
| 25 mM | 0.1022 mL | 0.5108 mL | 1.0216 mL | 2.5540 mL |