EPI-001 | Androgen Receptor Inhibitor | AmBeed-信号通路专用抑制剂

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EPI-001 {[allProObj[0].p_purity_real_show]}

货号：A201832

EPI-001是一种雄激素受体 N 末端结构域拮抗剂，IC50 约为 6 μM，同时也是一种选择性 PPAR-γ 调节剂。

EPI-001 化学结构
CAS号：227947-06-0

EPI-001 3D分子结构
CAS号：227947-06-0

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EPI-001 纯度/质量文件产品仅供科研

货号：A201832 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Adv. Funct. Mater., 2025, 2500696. Ambeed. [ A245395 ]; • JACS, 2025. Ambeed. [ A505336 ]; • Sci. Adv., 2025, 11(13): eadr0006. Ambeed. [ A152627 ]; • ACS Appl. Mater. Interfaces, 2025, 17(12): 18046-18058. Ambeed. [ A739356 , A171817 ]; • Food Res. Int., 2025, 116191. Ambeed. [ A1452012 ]; 更多 >

雄激素受体亚型比较

产品名称	Androgen Receptor ↓ ↑	纯度
Cyproterone acetate	++++ Androgen Receptor, IC50: 7.1 nM	98%
Apalutamide	+++ Androgen Receptor, IC50: 16 nM	98%
AZD3514	+ Androgen Receptor, Ki: 2.2 μM	99%
Darolutamide	++++ Androgen receptor, Ki: 11 nM	98%
Flutamide	+++ Androgen Receptor, Ki: 55 nM	98%
Galeterone	++ Androgen Receptor, IC50: 384 nM	98%
Enzalutamide	+++ Androgen Receptor, IC50: 36 nM	98%
Megestrol	✔	98%
Bicalutamide	++ Androgen Receptor, IC50: 0.16 μM	99%
EPI-001	+ Androgen Receptor, IC50: ~6 μM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

EPI-001 生物活性

靶点

Androgen Receptor

Androgen Receptor, IC50:~6 μM

描述

Androgen receptor (AR) is a member of the steroid hormone receptor family, and plays important role in the physiology and pathology of diverse tissues. EPI-001is an androgen receptor antagonist with an IC50 value of approximately 6μM for inhibition of transactivation of the androgen receptor N-terminal domain^[3]. EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5, and it also inhibits endogenous AR mRNA and protein expression. EPI-001(50 μM)is also a selective modulator of PPARγ in PCa cells^[4]. In vivo, EPI-001 blocks the androgen-axis and inhibits androgen-dependent tumor growth. Intravenous injection (i.v.) of EPI-001 (50mg/kg body weight) significantly reduced the weight of prostates from intact mice compared with control-treated animals. Similarly, LNCaP subcutaneous (s.c.) xenografts from intact male mice treated with EPI-001 by i.v. were significantly reduced in volume^[3].

EPI-001 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01839760	-		Completed	-	United States, Illinois ... 展开 >> Northwestern University Chicago, Illinois, United States, 60611 Australia, New South Wales Westmead Hospital Westmead, New South Wales, Australia, 2145 Australia, South Australia Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 Canada, Ontario North York General Hospital Toronto, Ontario, Canada, M2K 1E1 Mount Sinai Hospital Toronto, Ontario, Canada, M5G 1X5 收起 <<
NCT02188004	-		Completed	-	China, Guangxi ... 展开 >> Liuzhou Center of disease prevention and control Liuzhou, Guangxi, China 收起 <<
NCT02645396	-		Active, not recruiting	December 2018	China, Fujian ... 展开 >> Maternity and Child care of Huli District Xiamen, Fujian, China, 361000 China, Henan Maternity and Child care of Xinmi City Zhengzhou, Henan, China, 450000 收起 <<

EPI-001 参考文献

[1]Brand LJ, Olson ME, 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. Oncotarget. 2015 Feb 28;6(6):3811-24.

[2]Andersen RJ, Mawji NR, et al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell. 2010 Jun 15;17(6):535-46.

[3]Andersen RJ, Mawji NR, Wang J, et al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell. 2010;17(6):535-546.

[4]Brand LJ, Olson ME, Ravindranathan P, Guo H, Kempema AM, Andrews TE, Chen X, Raj GV, Harki DA, Dehm SM. EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer. Oncotarget. 2015 Feb 28;6(6):3811-24.

EPI-001 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.66mL

2.53mL

1.27mL

25.32mL

5.06mL

2.53mL

EPI-001 技术信息

CAS号	227947-06-0
分子式	C₂₁H₂₇ClO₅
分子量	394.89
SMILES Code	OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1
MDL No.	MFCD02683414

别名
运输	蓝冰
InChI Key	HDTYUHNZRYZEEB-UHFFFAOYSA-N
Pubchem ID	4166922

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 35 mg/mL(88.63 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

EPI-001 {[allProObj[0].p_purity_real_show]}

EPI-001 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

EPI-001 质控信息

EPI-001 生物活性

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EPI-001 参考文献

EPI-001 实验方案

EPI-001 技术信息

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EPI-001 {[allProObj[0].p_purity_real_show]}

EPI-001 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

EPI-001 质控信息

EPI-001 生物活性

EPI-001 临床研究

EPI-001 参考文献

EPI-001 实验方案

EPI-001 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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临床研究

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