Cyproterone acetate

Name: Cyproterone acetate
Brand: MedChemExpress
SKU: HY-13604
Rating: 5.0 (2 reviews)

Cat. No.: HY-13604 Purity: 99.19%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

Cyproterone acetate Chemical Structure

CAS No. : 427-51-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 72	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 72	In-stock	Estimated Time of Arrival: December 31
Solid
250 mg	USD 65	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
1 g		Get quote
5 g		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Cyproterone acetate:

Cyproterone acetate-d₃ Get quote
Cyproterone Acetate-¹³C₂,d₃ Get quote
Cyproterone acetate (Standard) Get quote

2 Publications Citing Use of MCE Cyproterone acetate

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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
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: 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	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	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: 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	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	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

Molecular Weight

416.94

Formula

C₂₄H₂₉ClO₄

CAS No.

427-51-0

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.19%

Select Batch:

Data Sheet (280 KB) SDS (392 KB)

COA (256 KB) HNMR (259 KB) RP-HPLC (89 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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