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Cat. No. Product Name CAS No. Information



Enobosarm (GTx-024, MK-2866, Ostarine) is a selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and osteoporosis.

Breast Cancer

Phase 2 Clinical


VPC 14449


VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression; effectively blocks transcriptional activity of full-length and splice variant AR forms at low to sub-micromolar concentrations; reduces tumor volume and abolishes PSA production in LNCaP xenograft model.




EPI-001 is a small molecule that blocks transactivation of the androgen Receptor (AR) NTD (IC50=6 uM) and specificly inhibits AR without attenuating transcriptional activities of related steroid receptors; targets the transactivation unit 5 of AR and interacts with AF-1 in the NTD to prevent protein-protein interactions; inhibits endogenous expression of androgen-regulated genes, inhibits both androgen-dependent and androgen-independent (OCM-induced) proliferation of LNCaP cells; reduces the growth of CRPC xenografts; also is a selective PPAR-gamma modulator.




BMS-641988 is a potent, selective, nonsteroidal androgen receptor antagonist with Ki of 1.7 nM, MDA-MB-453 cell IC50 of 16 nM; displays high selectivity over the glucocorticoid and progesterone receptors; displayed 3-7-fold increased antagonist activity of AR transactivation compared with bicalutamide; strongly inhibits androgen-dependent growth of the ventral prostate and seminal vesicles in rats, and is efficacious in CWR-22-BMSLD1 tumors initially refractory to treatment with bicalutamide.

Prostate Cancer

Phase 1 Clinical


GLPG-0492 R enantiomer


The R enantiomer of GLPG-0492, a non-steroidal selective androgen receptor modulator (SARM) for treatment for Duchenne muscular dystrophy (DMD); shows weak potency (1.25 uM) compared with GLPG-0492.




A novel, orally active, non-steroidal selective androgen receptor modulator (SARM) with in vitro potency of 13 nM; exhibits anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate in a classical model of orchidectomized rat; shows a potential treatment for Duchenne muscular dystrophy (DMD).

Other Indication

Phase 1 Clinical



IMTPPE (SID 3712502) is a novel small molecule capable of inhibiting androgen receptor (AR) transcriptional activity (IC50=1 uM) and protein level in C4-2 prostate cancer cells; IMTPPE inhibited proliferation of AR-positive, but not AR-negative, prostate cancer cells in culture. IMTPPE inhibited the transcriptional activity of a mutant AR lacking the ligand-binding domain (LBD); IMTPPE inhibited the growth of 22Rv1 xenograft tumor, a model for enzalutamide-resistant prostate cancer.

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