AR antagonist 3

Name: AR antagonist 3
Brand: MedChemExpress
SKU: HY-144127
Rating: 4.5 (1 reviews)

Cat. No.: HY-144127 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC₅₀ of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC₅₀= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally.

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

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 148	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 148	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 135	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 225	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 465	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC₅₀: 0.47 µM (AR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	IC₅₀	1.42 μM Compound: T1-12	Inhibition of prostate specific antigen expression in human LNCaP cells expressing ARR2PB-eGFP by immunoassay Inhibition of prostate specific antigen expression in human LNCaP cells expressing ARR2PB-eGFP by immunoassay	[PMID: 35077161]

In Vitro

AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 µM) shows excellent AR antagonistic activity (eGFP IC₅₀= 0.47 μM; PSA IC₅₀= 1.42 μM)^[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) inhibits the proliferation of LNCaP cells^[1].
AR antagonist 3 (0.1, 1, 10 µM; 48 h) reduces the protein expression levels of c-Myc and KLK3^[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) exhibits a dose-dependent decrease of the FRET signal (IC₅₀= 18.05 μM)^[1].
AR antagonist 3 (10 µM; 2 h) reduces the DHT-mediated translocation of the AR into the nucleus in LNCaP cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	LNCaP-ARR2PB-eGFP cells
Concentration:	0.01, 0.1, 1, 10, 100 µM
Incubation Time:
Result:	Showed excellent AR antagonistic activity (eGFP IC₅₀= 0.47 μM; PSA IC₅₀= 1.42 μM).

Cell Proliferation Assay^[1]

Cell Line:	LNCaP, 22Rv1, C4-2, PC3, DU145 cells
Concentration:	0.01, 0.1, 1, 10, 100 µM
Incubation Time:	3 days
Result:	Inhibited the proliferation of LNCaP cells.

In Vivo

AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65%^[1].

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

Animal Model:	6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g^[1]
Dosage:	2.5 mg/kg
Administration:	intratumorally injected; week; 25 days
Result:	Inhibited tumor growth and the final tumor growth inhibition is 65%.

Molecular Weight

306.38

Formula

C₁₅H₁₈N₂O₃S

CAS No.

349573-58-6

Appearance

Solid

Color

Light brown to brown

SMILES

CN(S(=O)(NC1=CC=C(C=C1)OCC2=CC=CC=C2)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (326.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2639 mL	16.3196 mL	32.6392 mL
5 mM	0.6528 mL	3.2639 mL	6.5278 mL
10 mM	0.3264 mL	1.6320 mL	3.2639 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (8.16 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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 (8.16 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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 (8.16 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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.

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: 99.96%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (247 KB) HNMR (120 KB) RP-HPLC (168 KB) LCMS (388 KB)

Handling Instructions (2659 KB)

References

[1]. Chai X, et al. Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2. J Med Chem. 2022, 65(3):2507-2521. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.2639 mL	16.3196 mL	32.6392 mL	81.5980 mL
	5 mM	0.6528 mL	3.2639 mL	6.5278 mL	16.3196 mL
	10 mM	0.3264 mL	1.6320 mL	3.2639 mL	8.1598 mL
	15 mM	0.2176 mL	1.0880 mL	2.1759 mL	5.4399 mL
	20 mM	0.1632 mL	0.8160 mL	1.6320 mL	4.0799 mL
	25 mM	0.1306 mL	0.6528 mL	1.3056 mL	3.2639 mL
	30 mM	0.1088 mL	0.5440 mL	1.0880 mL	2.7199 mL
	40 mM	0.0816 mL	0.4080 mL	0.8160 mL	2.0400 mL
	50 mM	0.0653 mL	0.3264 mL	0.6528 mL	1.6320 mL
	60 mM	0.0544 mL	0.2720 mL	0.5440 mL	1.3600 mL
	80 mM	0.0408 mL	0.2040 mL	0.4080 mL	1.0200 mL
	100 mM	0.0326 mL	0.1632 mL	0.3264 mL	0.8160 mL

AR antagonist 3 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AR antagonist 3349573-58-6AR antagonist3AR antagonist-3Androgen ReceptoranticancerLNCaP cellsc-MycKLK3selectiveFRETLNCaP xenograftInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

AR antagonist 3

Customer Review

AR antagonist 3 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

AR antagonist 3 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AR antagonist 3 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report