2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. AR antagonist 3

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.

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AR antagonist 3 Chemical Structure

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 148 In-stock
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10 mM * 1 mL in DMSO USD 148 In-stock
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5 mg USD 135 In-stock
10 mg USD 225 In-stock
25 mg USD 465 In-stock
50 mg USD 790 In-stock
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Based on 1 publication(s) in Google Scholar

AR antagonist 3 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 0.47 µM (AR)[1]
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.

AR antagonist 3 Related Antibodies

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.
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
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)

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(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
References

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.

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
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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

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