Androgen Receptor

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
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 Apalutamide (ARN-509) <1 mg/mL 18 mg/mL 5 mg/mL
S1140 Andarine <1 mg/mL 88 mg/mL 88 mg/mL
S2803 Galeterone <1 mg/mL 24 mg/mL 40 mg/mL
S1908 Flutamide <1 mg/mL 55 mg/mL 55 mg/mL
S2604 Dehydroepiandrosterone (DHEA) <1 mg/mL 57 mg/mL 57 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
S2832 Epiandrosterone <1 mg/mL 29 mg/mL 58 mg/mL
S7040 AZD3514 <1 mg/mL 100 mg/mL 100 mg/mL
S4054 Spironolactone <1 mg/mL 83 mg/mL 20 mg/mL
S4593 Chlormadinone acetate <1 mg/mL 27 mg/mL 1 mg/mL
S7559 ODM-201 <1 mg/mL 80 mg/mL 38 mg/mL
S7955 EPI-001 <1 mg/mL 79 mg/mL 79 mg/mL
Catalog No. Information Product Use Citations Product Validations
S2840

Apalutamide (ARN-509)

Apalutamide (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.

S1304

Megestrol Acetate

Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.

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.

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.

S1140

Andarine

Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.

S2832

Epiandrosterone

Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.

S1250

Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

S1190

Bicalutamide

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.

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.

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.

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

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.

S4054

Spironolactone

Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.

S4593

Chlormadinone acetate

Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

S7559

ODM-201

ODM-201 is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.

S7955

EPI-001

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

Catalog No. Information Product Use Citations Product Validations
S2840

Apalutamide (ARN-509)

Apalutamide (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.

S1304

Megestrol Acetate

Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.

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.

Catalog No. Information Product Use Citations Product Validations
S1250

Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

2017, 355(6320):78-83

2017, 355(6320):84-88

2015, 10.1093/nar/gkv262

S1190

Bicalutamide

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.

2014, 10.1038/onc.2014.302

2014, 10.1158/1535-7163.MCT-14-0819

2012, 131(6):E872-83

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.

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.

2014, 10.1158/1535-7163.MCT-14-0819

2016, 104(9):2345-55

2017, 37(8):933-942

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

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.

S4054

Spironolactone

Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.

S4593

Chlormadinone acetate

Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

S7559

ODM-201

ODM-201 is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.

S7955

EPI-001

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

Catalog No. Information Product Use Citations Product Validations
S1140

Andarine

Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.

2013, 30(9):1517-26

S2832

Epiandrosterone

Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.

Catalog No. Information Product Use Citations Product Validations
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.

2013, 84:278-84

2011, 3(5):331-6