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Cat. No. Product Name CAS No. Information
PC-62000

Enobosarm

841205-47-8

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

PC-61774

VPC 14449

1621375-32-3

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.

PC-61678

EPI-001

227947-06-0

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.

PC-61086

BMS-641988

573738-99-5

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

PC-35680

KCI807

6665-68-5 KCI807 (KCI-807) is a lead molecule that selectively disrupts ELK1-dependent promoter activation by wild-type and variant Ars (IC50=0.53 uM) without interfering with ELK1 activation by ERK; binds to AR (Kd=69.2 nM), blocking ELK1 binding, and selectively blocks recruitment of AR to chromatin by ELK1; primarily affects a subset of AR target growth genes selectively suppressing AR-dependent growth of PC cell lines with a better inhibitory profile than Enzalutamide; also inhibits in vivo growth of castration/enzalutamide-resistant cell line-derived and patient-derived tumor xenografts.
PC-35497

Leelamine hydrochloride

16496-99-4 Leelamine hydrochloride (Dehydroabietylamine) is a novel inhibitor of androgen receptor (AR), inhibits castration-resistant prostate cancer cells; causes apoptosis and suppresses 22Rv1 xenograft growth in vivo; Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport.
PC-35346

RD162

915087-27-3 RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM; suppresses growth and induces apoptosis in human prostate cancer cells in vitro, demonstrates greater relative affinity than the clinically used antiandrogen bicalutamide, reduces the efficiency of its nuclear translocation, and impairs both DNA binding to androgen response elements and recruitment of coactivators; induces tumor regression in mouse models of castration-resistant human prostate cancer.

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