您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > EPI-001
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
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
包装与价格:
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
EPI-001 是一种雄激素受体 (AR) 的选择性抑制剂,靶向 AR 的反式激活单元 5 (Tau-5)。 EPI-001 可以抑制 AR 氨基末端结构域 (NTD) 的反式激活,IC50 约为 6 μM。 EPI-001 也是 PPARγ 的选择性调节剂。 EPI-001 对去势抵抗性前列腺癌有活性。
Cas No.227947-06-0
别名双酚A
化学名3-(4-(2-(4-(3-chloro-2-hydroxypropoxy)phenyl)propan-2-yl)phenoxy)propane-1,2-diol
Canonical SMILESCC(C1=CC=C(OCC(O)CCl)C=C1)(C2=CC=C(OCC(O)CO)C=C2)C
分子式C21H27ClO5
分子量394.89
溶解度≥ 19.75mg/mL in DMSO with ultrasonic
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
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.