Art. -Nr.: HY-13604

Cyproterone acetate

3 Cited Publications

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Cyproterone acetate is an anti-androgen (IC₅₀=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors.

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Reinheit: 99.90%
CAS. Nr.: 427-51-0
Formel: C₂₄H₂₉ClO₄
Molecular Weight:416.94

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cyproterone acetate Chemical Structure

CAS. Nr.: 427-51-0

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cyproterone acetate is an anti-androgen (IC₅₀=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
CV-1	IC₅₀	23 nM Compound: 1	Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells.	[PMID: 9484511]
CV-1	IC₅₀	>1000 nM Compound: 1	Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells.	[PMID: 9484511]
DU-145	IC₅₀	50.7 μM Compound: CPA	Antiproliferative activity against androgen-insensitive human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against androgen-insensitive human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 33933755]
LNCaP	IC₅₀	43 μM Compound: Cyproterone acetate	Cytotoxicity against human androgen receptor positive LNCAP cells after 72 hrs by MTT assay Cytotoxicity against human androgen receptor positive LNCAP cells after 72 hrs by MTT assay	[PMID: 20226660]
LNCaP	IC₅₀	43 μM Compound: CPA	Cytotoxicity against human LNCAP cells expressing androgen receptor after 72 hrs by MTT assay Cytotoxicity against human LNCAP cells expressing androgen receptor after 72 hrs by MTT assay	[PMID: 23665800]
LNCaP	IC₅₀	59.6 μM Compound: CPA	Antiproliferative activity against androgen-sensitive human LNCaP cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against androgen-sensitive human LNCaP cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 33933755]
PC-3	IC₅₀	32.3 μM Compound: Cyproterone acetate	Cytotoxicity against human androgen receptor negative PC3 cells after 72 hrs by MTT assay Cytotoxicity against human androgen receptor negative PC3 cells after 72 hrs by MTT assay	[PMID: 20226660]
PC-3	IC₅₀	32.3 μM Compound: CPA	Cytotoxicity against androgen receptor deficient human PC3 cells after 72 hrs by MTT assay Cytotoxicity against androgen receptor deficient human PC3 cells after 72 hrs by MTT assay	[PMID: 23665800]
PC-3	IC₅₀	56.9 μM Compound: CPA	Antiproliferative activity against androgen-insensitive human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against androgen-insensitive human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 33933755]

In Vitro

Cyproterone acetate is a partial agonist, showing agonism for the AR, with EC₅₀ of 4.0 μM, at relatively high concentrations^[1].
Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5^[3].
Cyproterone acetate pretreatment (0,1,10, or 50 μM; 24 hours; subsequently exposed to cadmium for an additional 24 hours) resulted in a clear decrease in the sensitivity to cadmium in rat liver epithelial cell line^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Adult male C57 BL/6J mice injected with 0.08 mg/g of cyproterone acetate showed an increase in cellular lipid content in the zona fasciculata and zona retjculans of the adrenal cortex^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 427-51-0
Appearance Solid
Molecular Weight 416.94
Formel C₂₄H₂₉ClO₄
Color White to off-white
SMILES

C[C@]12[C@]3([H])[C@@](C(C=C1C(Cl)=C[C@]4([H])[C@]2([H])CC[C@]5([C@@]4([H])CC[C@@]5(C(C)=O)OC(C)=O)C)=O)([H])C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Int J Mol Sci

Metformin Enhances Nomegestrol Acetate Suppressing Growth of Endometrial Cancer Cells and May Correlate to Downregulating mTOR Activity In Vitro and In Vivo. [Abstract]

2019 Jul 5;20(13):3308. PMID: 31284427
Medicina (Kaunas)

2025.
Charles University

2020 Jul.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (79.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 20 mg/mL (47.97 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3984 mL

11.9921 mL

23.9843 mL

5 mM

0.4797 mL

2.3984 mL

4.7969 mL

10 mM

0.2398 mL

1.1992 mL

2.3984 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline

Solubility: 2 mg/mL (4.80 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (20.0 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.

Protocol 5

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2 mg/mL (4.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 6

Add each solvent one by one: 10% EtOH 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sonneveld, E., et al., Development of androgen- and estrogen-responsive bioassays, members of a panel of human cell line-based highly selective steroid-responsive bioassays. Toxicol Sci, 2005. 83(1): p. 136-48. [Content Brief]

[2]. Torri V,. Cyproterone acetate in the therapy of prostate carcinoma. Arch Ital Urol Androl. 2005;77(3):157-163. [Content Brief]

[3]. Chen L, et al. Cyproterone acetate enhances TRAIL-induced androgen-independent prostate cancer cell apoptosis via up-regulation of death receptor 5. BMC Cancer. 2017;17(1):179. Published 2017 Mar 7. [Content Brief]

[4]. Takiguchi M, et al. Cyproterone acetate induces a cellular tolerance to cadmium in rat liver epithelial cells involving reduced cadmium accumulation. Toxicology. 2001;165(1):13-25. [Content Brief]

[5]. Migally N. Effect of cyproterone acetate on the structure of the adrenal cortex. Arch Androl. 1979;2(2):109-115. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
Ethanol / DMSO	1 mM	2.3984 mL	11.9921 mL	23.9843 mL	59.9607 mL
	5 mM	0.4797 mL	2.3984 mL	4.7969 mL	11.9921 mL
	10 mM	0.2398 mL	1.1992 mL	2.3984 mL	5.9961 mL
	15 mM	0.1599 mL	0.7995 mL	1.5990 mL	3.9974 mL
	20 mM	0.1199 mL	0.5996 mL	1.1992 mL	2.9980 mL
	25 mM	0.0959 mL	0.4797 mL	0.9594 mL	2.3984 mL
	30 mM	0.0799 mL	0.3997 mL	0.7995 mL	1.9987 mL
	40 mM	0.0600 mL	0.2998 mL	0.5996 mL	1.4990 mL
DMSO	50 mM	0.0480 mL	0.2398 mL	0.4797 mL	1.1992 mL
DMSO	60 mM	0.0400 mL	0.1999 mL	0.3997 mL	0.9993 mL

Keywords

Cyproterone acetate

3 Cited Publications

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Cyproterone acetate

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Publications Citing Use of MedChemExpress (MCE) Cyproterone acetate

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cyproterone acetate

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Endocrinology Compound Library

NMPA-Approved Drug Library

FDA Approved & Pharmacopeial Drug Library

Transcription Factor-Targeted Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Anti-Aging Natural Product Library

Off-patent Drug Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Human Hormone Compound Library

Steroid Hormones Library

Publications Citing Use of MedChemExpress (MCE) Cyproterone acetate

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cyproterone acetate Related Classifications

HY-13604 Related Classifications