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Androgen receptor antagonist 1

🥰Excellent
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

🥰Excellent
Purity: 99.054%
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. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:99.054%
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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)
ColorWhite
AppearanceSolid
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 recommeded.
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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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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2 Enter the in vivo formulation:
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Keywords

androgen receptor
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