Biological Activity
EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in vivo[1][2].
In Vitro
EPI-001 (5-100 μM; 7 d) inhibits PCa/CRPC cell growth in a dose-dependent manner[2]. EPI-001 (50 μM) inhibits endogenous AR mRNA and protein expression in PCa and CRPC cell lines[2]. EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5[2]. Cell Proliferation Assay[2] Cell Line: PCa, CRPC, PC-3, DU 145, and T47D cell lines Concentration: 0, 5, 10, 25, 50, 100 μM Incubation Time: 7 days Result: Inhibited growth of LNCaP cells at low concentrations. Inhibited growth of AR-negative PC-3 and DU 145 cell lines as well as the T47D breast carcinoma cell line. Western Blot Analysis[2] Cell Line: LNCaP, VCaP LAPC4, C4-2,22Rv1, and CWR-R1 cells Concentration: 50 μM Incubation Time: 8-16 hours Result: Decreased expression of full-length AR protein to varying degrees.
In Vivo
EPI-00 (20 mg/kg; i.v. every 5 d for 25 d) inhibits the growth of tumors and has no general toxicity in vivo[1]. EPI-00 (50 mg/kg; i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth[1]. Animal Model: Male NOD-SCID mice (6-8 weeks) bearing LNCaP[1] Dosage: 20 mg/kg Administration: I.v. every 5 days for 25 days Result: Reduced tumors from 100.3±1.72 mm3 to 73.03±29.6 mm3 within 2 weeks. Did not cause general toxicity indicated by no change in animal behavior or body weight.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.