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EPI-001

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Chemical Structure| 227947-06-0 同义名 : -
CAS号 : 227947-06-0
货号 : A201832
分子式 : C21H27ClO5
纯度 : 98%
分子量 : 394.889
MDL号 : MFCD02683414
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
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 <<
实验方案
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
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.