Androgen Receptor Antagonists

Cat.No.	Product Name	Information	Product Use Citations
S1250	MDV3100 (Enzalutamide)	Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.	Cancer Cell, 2025, 43(5):891-904.e10 Nat Genet, 2025, 57(10):2468-2481 Nat Genet, 2025, 57(12):3027-3038
S1190	Bicalutamide	Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. This compound promotes autophagy.	Nat Commun, 2025, 16(1):6587 Nat Commun, 2025, 16(1):6451 J Control Release, 2025, 380:417-432
S2840	ARN-509 (Apalutamide)	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.	Nat Genet, 2025, 57(12):3027-3038 Nat Commun, 2025, 16(1):6587 J Control Release, 2025, 380:417-432
S1908	Flutamide	Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i values of 55 nM, and this compound is primarily used to treat prostate cancer.	iScience, 2024, 27(10):110862 Zool Res, 2024, 45(2):355-366 Dis Model Mech, 2024, 17(10)dmm050900
S7559	ODM-201 (Darolutamide)	Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.	Nat Commun, 2025, 16(1):6587 Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812 Cell Rep, 2025, 44(6):115779
S4054	Spironolactone	Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.	Cancer Cell, 2025, 43(4):776-796.e14 J Clin Invest, 2025, 135(16)e187663 Biomed Pharmacother, 2024, 180:117523
S7955	EPI-001	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.	Int J Biol Macromol, 2024, 278(Pt 3):134844 Nat Struct Mol Biol, 2023, 30(12):1958-1969 Int J Mol Sci, 2023, 24(4)3823
S2803	Galeterone	Galeterone (TOK-001) 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.	ChemMedChem, 2022, e202200043 Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w Steroids, 2020, 153:108534
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.	iScience, 2024, 110862 iScience, 2024, 27(10):110862 Sci Rep, 2021, 11(1):5457
S4728	3,3'-Diindolylmethane	3,3'-Diindolylmethane (DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. This compound is a strong, pure androgen receptor (AR) antagonist.	FASEB J, 2021, 35(5):e21502 Cell Death Dis, 2019, 10(2):38
S9898	Proxalutamide (GT0918)	Proxalutamide (GT0918), a second-generation androgen receptor antagonist, binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.	CNS Neurosci Ther, 2024, 30(6):e14822
E1502	Deutenzalutamide	Deutenzalutamide (HC-1119, MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. It can be used in a treatment of advanced prostate cancer.
S4836	Nilutamide	Nilutamide (RU23908) 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 (Gestafortin) 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.
S9900	JNJ-63576253 (TRC-253)	JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM, and it displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.
S8885	UT-34	UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. This compound is a potential next-generation therapeutic for -resistant prostate cancer.
S5285	RU58841	RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
E1964	BMS-986365	BMS-986365 (CC-94676) is a potent and selective, heterobifunctional ligand-directed degrader (LDD) and antagonist of androgen receptor (AR), that effectively targets both wildtype and mutant forms of the androgen receptor (AR) in the cytoplasm and nucleus. It rapidly degrades AR, suppresses AR signaling, and shows promising clinical activity in inhibiting tumor growth in patients with metastatic castration-resistant prostate cancer (mCRPC).
E0608	Pyrilutamide (KX-826)	Pyrilutamide (KX-826) is an antagonist of androgen receptor (AR) and a potential first-in-class topical drug for the treatment of androgenetic alopecia (AGA) and acne vulgaris.
S9045	Triptophenolide	Triptophenolide (Hypolide), 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.
E2850	ORM-15341	ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 value of 38 nM and the inhibition constant (Ki) value of 8 nM.
S6896	Clascoterone	Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) is a topical and peripherally selective antagonist of androgen receptor (AR).
S5437	4,4'-DDE	4,4'-DDE (DDE, p,p'-DDE, p,p'-dichlorodiphenyldichloroethylene), a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.