Androgen Receptor

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Androgen Receptor Inhibitors | Agonists | Antagonists | Modulators (15)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1250 Enzalutamide (MDV3100) Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
  • Nucleic Acids Res, 2015, 10.1093/nar/gkv262
  • Int J Cancer, 2012, 131(6):E872-83
  • Am J Pathol, 2013, 182(2):460-73
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.
  • Oncogene, 2014, 10.1038/onc.2014.302
  • Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0819
  • Int J Cancer, 2012, 131(6):E872-83
S1174 MK-2866 (GTx-024) MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
  • J Pharm Biomed Anal, 2013, 84:278-84
  • Drug Test Anal, 2011, 3(5):331-6
S2840 ARN-509 ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
  • J Cancer, 2014, 5(2):133-42
S1140 Andarine Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.
  • Food Addit Contam A, 2013, 30(9):1517-26
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
S2803 Galeterone Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
  • Biochem Biophys Res Commun, 2016, 477(4):1005-10
S1908 Flutamide Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
  • Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0819
S7559 ODM-201 ODM-201 is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
S7040 AZD3514 AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
S2604 Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
S2832 Epiandrosterone Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
S2042 Cyproterone Acetate Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.
S1304 Megestrol Acetate Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.
S4054 Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1250 Enzalutamide (MDV3100) <1 mg/mL 92 mg/mL <1 mg/mL
S1190 Bicalutamide <1 mg/mL 86 mg/mL 5 mg/mL
S1174 MK-2866 (GTx-024) <1 mg/mL 78 mg/mL 78 mg/mL
S2840 ARN-509 <1 mg/mL 18 mg/mL 5 mg/mL
S1140 Andarine <1 mg/mL 88 mg/mL 88 mg/mL
S7955 EPI-001 <1 mg/mL 79 mg/mL 79 mg/mL
S2803 Galeterone <1 mg/mL 24 mg/mL 40 mg/mL
S1908 Flutamide <1 mg/mL 55 mg/mL 55 mg/mL
S7559 ODM-201 <1 mg/mL 80 mg/mL 38 mg/mL
S7040 AZD3514 <1 mg/mL 100 mg/mL 100 mg/mL
S2604 Dehydroepiandrosterone (DHEA) <1 mg/mL 57 mg/mL 57 mg/mL
S2832 Epiandrosterone <1 mg/mL 29 mg/mL 58 mg/mL
S2042 Cyproterone Acetate <1 mg/mL 83 mg/mL 10 mg/mL
S1304 Megestrol Acetate <1 mg/mL 33 mg/mL 15 mg/mL
S4054 Spironolactone <1 mg/mL 83 mg/mL 20 mg/mL
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