EPI-001

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EPI-001 是一种小分子，可阻断雄激素受体 (AR) NTD 的反式激活 (IC50=6 uM)。

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.

Cell Proliferation Assay 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 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.

Animal Model:Male NOD-SCID mice (6-8 weeks) bearing LNCaP 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.

EPI001

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor

Cancer

——

227947-06-0

394.89

C21H27ClO5

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (84.40 mM)

OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1

3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol

(-20℃)

With Ice Pack

≥ 2 years