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Androgen receptor antagonist 1

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Catalog No. T10320Cas No. 1338812-36-4

Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.

Androgen receptor antagonist 1

Androgen receptor antagonist 1

😃Good
Purity: 99.05%
Catalog No. T10320Cas No. 1338812-36-4
Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$148-In Stock
5 mg$372-In Stock
10 mg$662-In Stock
25 mg$1,280-In Stock
50 mg$1,930-In Stock
1 mL x 10 mM (in DMSO)$397-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:99.05%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.
Targets&IC50
Androgen receptor:59 nM
In vitro
Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) demonstrates significant cell growth inhibition in LNAR and LNCaP cells, but not in DU145 cells [1].
In vivo
Androgen receptor antagonist 1 (100 mg/kg once a day for 5 weeks) shows excellent in vivo tumor growth inhibition upon oral administration in castration-resistant prostate cancer (CRPC) animal model [1].
Chemical Properties
Molecular Weight416.9
FormulaC21H25ClN4O3
Cas No.1338812-36-4
SmilesCC1(C)[C@H](NC(=O)c2cnn(CCO)c2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1
Relative Density.1.30 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (191.89 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 3.3 mg/mL (7.92 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3987 mL11.9933 mL23.9866 mL119.9328 mL
5 mM0.4797 mL2.3987 mL4.7973 mL23.9866 mL
10 mM0.2399 mL1.1993 mL2.3987 mL11.9933 mL
20 mM0.1199 mL0.5997 mL1.1993 mL5.9966 mL
50 mM0.0480 mL0.2399 mL0.4797 mL2.3987 mL
100 mM0.0240 mL0.1199 mL0.2399 mL1.1993 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

androgen receptor
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