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EPI-001
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EPI-001图片
CAS NO:227947-06-0
规格:98%
分子量:394.89
包装与价格:
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
AR antagonist
CAS:227947-06-0
分子式:C21H27ClO5
分子量:394.89
纯度:98%
存储:Store at -20°C

Background:

EPI-001 is a small-molecule inhibitor of androgen receptor N-terminal domain. EPI-001 could target the amino terminal domain of the AR and inhibit the protein-protein interactions which are necessary for AR transcriptional activity. The androgen receptor (AR) is involved in mediating the actions of male sex steroids. Amplification and over-expression of androgen receptor gene may result in hormone-refractory prostate cancer [1].


In vitro: EPI-001 inhibited the ligand-dependent ARGal4 transcriptional activity in LNCaP cells and the ligand-independent ARGal4 transcriptional activity in the CRPC C4-2 cell line. In a panel of cell lines, EPI-001 treatment decreased the mRNA expression level of AR protein after 8 and 16 h treatment, such as androgen sensitive PCa, CRPC, LNCap, C4-2, and LAPC4 cell line. EPI-001 dose-dependently inhibited the PCa/CRPC cell growth [2].


In vivo: Intravenous injection of EPI-001 significantly reduced the weight of benign prostates and blocked the growth of prostate cancer xenograft from noncastrated mature mice. EPI-001 caused tumor regression of CRPC. In male mice bearing LNCaP xenografts, after treated with EPI- 001 by i.v. injection for 2 weeks, the tumor size was less than half of the control group [3].


参考文献:
Andersen R J, Mawji N R, Wang J, et al.  Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor[J]. Cancer cell, 2010, 17(6): 535-546.
Brand L J, Olson M E, Ravindranathan P, et al.  EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer[J]. Oncotarget, 2015, 6(6): 3811.
Sadar M D.  Small molecule inhibitors targeting the “achilles' heel” of androgen receptor activity[J]. Cancer research, 2011, 71(4): 1208-1213.