Androgen Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S2840	Apalutamide (ARN-509)	<1 mg/mL	18 mg/mL	5 mg/mL
S1304	Megestrol Acetate	<1 mg/mL	33 mg/mL	15 mg/mL
S7040	AZD3514	<1 mg/mL	100 mg/mL	100 mg/mL
S4797	Nicergoline	-1 mg/mL	22 mg/mL	-1 mg/mL
S1250	Enzalutamide (MDV3100)	<1 mg/mL	92 mg/mL	<1 mg/mL
S1190	Bicalutamide	<1 mg/mL	86 mg/mL	5 mg/mL
s9045	Triptophenolide	-1 mg/mL	62 mg/mL	-1 mg/mL
S5285	RU58841	<1 mg/mL	73 mg/mL	73 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
S4054	Spironolactone	<1 mg/mL	83 mg/mL	20 mg/mL
S4836	Nilutamide	<1 mg/mL	63 mg/mL	63 mg/mL
S4593	Chlormadinone acetate	<1 mg/mL	27 mg/mL	1 mg/mL
S7559	Darolutamide (ODM-201)	<1 mg/mL	80 mg/mL	38 mg/mL
S7955	EPI-001	<1 mg/mL	79 mg/mL	79 mg/mL
S1140	Andarine	<1 mg/mL	88 mg/mL	88 mg/mL
S6352	Androsterone	-1 mg/mL	29 mg/mL	-1 mg/mL
S2832	Epiandrosterone	<1 mg/mL	29 mg/mL	58 mg/mL
S3946	Mesterolone	-1 mg/mL	13 mg/mL	-1 mg/mL
S4794	Drostanolone Propionate	-1 mg/mL	18 mg/mL	-1 mg/mL
S4795	Trenbolone acetate	-1 mg/mL	62 mg/mL	-1 mg/mL
S3717	Testosterone Enanthate	9 mg/mL	80 mg/mL	80 mg/mL
S4757	Dihydrotestosterone(DHT)	<1 mg/mL	58 mg/mL	58 mg/mL
S1174	Ostarine (GTx-024, MK-2866 )	<1 mg/mL	78 mg/mL	78 mg/mL
S5275	Testolone (RAD140)	-1 mg/mL	78 mg/mL	-1 mg/mL

Androgen Receptor Products

All (29) Androgen Receptor Inhibitors (4) Androgen Receptor Antagonists (13) Androgen Receptor Agonists (10) Androgen Receptor Modulators (2) New Androgen Receptor Products

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.	Cancer Cell Int, 2018, 18:71 J Cancer, 2014, 5(2):133-42 Clin Cancer Res, 2017, 23(24):7608-7620	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
S1304	Megestrol Acetate Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.	Onco Targets Ther, 2017, 10:4809-4819 Sci Rep, 2017, 7(1):12754	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514 is a potent and oral androgen receptor downregulator with K_i of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
S4797	Nicergoline Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.
S1250	Enzalutamide (MDV3100) Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.	Science, 2017, 355(6320):78-83 Science, 2017, 355(6320):84-88 Nat Med, 2018, 24(2):239-246	Survival of mice receiving daily vehicle or MDV3100 treatment and treated with the LHRH-Ant or vehicle (n=10 mice per group). Data combined from two independent experiments.
S1190	Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.	Cancer Res, 2018, 10.1158/0008-5472.CAN-17-3728 Cancer Res, 2018, 78(13):3659-3671 Int J Cancer, 2012, 131(6):E872-83
s9045^New	Triptophenolide Triptophenolide, derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S5285^New	RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
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 Steroids, 2018, 138:82-90	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i values of 55 nM, and primarily used to treat prostate cancer.	Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0819 J Biomed Mater Res A, 2016, 104(9):2345-55 J Appl Toxicol, 2017, 37(8):933-942	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
S2604	Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.	Cancer Lett, , 382(2):195-202
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.	Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
S4054	Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.	Antiviral Res, 2017, 146:76-85 Environ Pollut, 2018, 234:846-854 Leukemia, 2018, 32(1):111-119	(A, B) Indicated HIV-1 latency cells (A. J-LAT 10.6; B. CA5) were treated with levosimendan or spironolactone (5, 10, or 20 μM) in combination with TNFα (10 ng/ml). After 24 hr, mRNA was extracted, and reverse transcribed to cDNA for measurement of HIV-1 initiated or elongated (proximal [Pro], intermediate [Int], and distal [Dis]) transcripts by qPCR. Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6).
S4836	Nilutamide Nilutamide is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.
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	Darolutamide (ODM-201) Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.	Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1469	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
S7955	EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
S1140	Andarine Andarine is a selective non-steroidal androgen receptor (AR) agonist with K_i of 4 nM, tissue-selective for anabolic organs. Phase 3.	Food Addit Contam A, 2013, 30(9):1517-26 J Pharm Biomed Anal, 2018, 158:189-203 J Chromatogr A, 2017, 1490:89-101
S6352^New	Androsterone Androsterone is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.
S2832	Epiandrosterone Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
S3830	Protodioscin Protodioscin, a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946	Mesterolone Mesterolone is a synthetic steroid with anabolic and androgenic activities.
S4794	Drostanolone Propionate Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate Trenbolone acetate, a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S3717	Testosterone Enanthate Testosterone Enanthate is an androgen and anabolic steroid used in androgen replacement therapy.
S3715	Boldenone Undecylenate Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.
S4757	Dihydrotestosterone(DHT) Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.
S1174	Ostarine (GTx-024, MK-2866 ) MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.	Drug Test Anal, 2011, 3(5):331-6 J Pharm Biomed Anal, 2013, 84:278-84
S5275^New	Testolone (RAD140) RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

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.	Cancer Cell Int, 2018, 18:71 J Cancer, 2014, 5(2):133-42 Clin Cancer Res, 2017, 23(24):7608-7620	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
S1304	Megestrol Acetate Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.	Onco Targets Ther, 2017, 10:4809-4819 Sci Rep, 2017, 7(1):12754	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514 is a potent and oral androgen receptor downregulator with K_i of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
S4797	Nicergoline Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.

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.	Science, 2017, 355(6320):78-83 Science, 2017, 355(6320):84-88 Nat Med, 2018, 24(2):239-246	Survival of mice receiving daily vehicle or MDV3100 treatment and treated with the LHRH-Ant or vehicle (n=10 mice per group). Data combined from two independent experiments.
S1190	Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.	Cancer Res, 2018, 10.1158/0008-5472.CAN-17-3728 Cancer Res, 2018, 78(13):3659-3671 Int J Cancer, 2012, 131(6):E872-83
s9045^New	Triptophenolide Triptophenolide, derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S5285^New	RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
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 Steroids, 2018, 138:82-90	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i values of 55 nM, and primarily used to treat prostate cancer.	Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0819 J Biomed Mater Res A, 2016, 104(9):2345-55 J Appl Toxicol, 2017, 37(8):933-942	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
S2604	Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.	Cancer Lett, , 382(2):195-202
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.	Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
S4054	Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.	Antiviral Res, 2017, 146:76-85 Environ Pollut, 2018, 234:846-854 Leukemia, 2018, 32(1):111-119	(A, B) Indicated HIV-1 latency cells (A. J-LAT 10.6; B. CA5) were treated with levosimendan or spironolactone (5, 10, or 20 μM) in combination with TNFα (10 ng/ml). After 24 hr, mRNA was extracted, and reverse transcribed to cDNA for measurement of HIV-1 initiated or elongated (proximal [Pro], intermediate [Int], and distal [Dis]) transcripts by qPCR. Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6).
S4836	Nilutamide Nilutamide is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.
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	Darolutamide (ODM-201) Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.	Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1469	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
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
S1140	Andarine Andarine is a selective non-steroidal androgen receptor (AR) agonist with K_i of 4 nM, tissue-selective for anabolic organs. Phase 3.	Food Addit Contam A, 2013, 30(9):1517-26 J Pharm Biomed Anal, 2018, 158:189-203 J Chromatogr A, 2017, 1490:89-101
S6352^New	Androsterone Androsterone is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.
S2832	Epiandrosterone Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
S3830	Protodioscin Protodioscin, a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946	Mesterolone Mesterolone is a synthetic steroid with anabolic and androgenic activities.
S4794	Drostanolone Propionate Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate Trenbolone acetate, a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S3717	Testosterone Enanthate Testosterone Enanthate is an androgen and anabolic steroid used in androgen replacement therapy.
S3715	Boldenone Undecylenate Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.
S4757	Dihydrotestosterone(DHT) Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.

Catalog No.	Information	Product Use Citations	Product Validations
S1174	Ostarine (GTx-024, MK-2866 ) MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.	Drug Test Anal, 2011, 3(5):331-6 J Pharm Biomed Anal, 2013, 84:278-84
S5275^New	Testolone (RAD140) RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

Catalog No.

Information

Product Use Citations

Product Validations

S1174

Ostarine (GTx-024, MK-2866 )

MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

Drug Test Anal, 2011, 3(5):331-6

J Pharm Biomed Anal, 2013, 84:278-84

S5275^New

Testolone (RAD140)

RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

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Androgen Receptor

Signaling Pathway Map

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Androgen Receptor Products