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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 SizePriceAvailabilityQuantity
1 mg$148In Stock
5 mg$372In Stock
10 mg$662In Stock
25 mg$1,280In Stock
50 mg$1,930In Stock
1 mL x 10 mM (in DMSO)$397In Stock
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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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COA HNMR LCMS

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.
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:
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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.
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Keywords

androgen receptor
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