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 reduced lipid accumulation in hepatic cells
Int J Mol Sci. 2022 Dec 16;23(24):16063.
LNCaP cells
50 μM
Inhibition of AR transcriptional activity
Oncotarget. 2015 Feb 28;6(6):3811-24.
293T cells
50 μM
Inhibition of AR transcriptional activity
Oncotarget. 2015 Feb 28;6(6):3811-24.
C4-2 cells
50 μM
Inhibition of AR transcriptional activity
Oncotarget. 2015 Feb 28;6(6):3811-24.
LNCaP cells
25 μM
48 hours
EPI-001 inhibited AR transcriptional activity consistently, regardless of increasing levels of androgen, and at 50 nM R1881, EPI-001 still inhibited AR activity by approximately 80%.
J Clin Invest. 2013 Jul;123(7):2948-60.
CV-1 monkey kidney cells
5 μM
48 hours
To evaluate the effect of EPI-001 on AR transcriptional activity. Results showed EPI-001 did not inhibit gene transcription at 5 μM concentration.
ChemMedChem. 2023 Jan 17;18(2):e202200548.
C4-2b prostate cancer cells
1.7-4.6 μM
72 hours
To evaluate the cytotoxic effects of EPI-001 and its derivatives on C4-2b cells. Results showed EPI-001 had an LC50 of 84.4 μM, while derivatives exhibited higher toxicity (LC50 1.7-4.6 μM).
ChemMedChem. 2023 Jan 17;18(2):e202200548.
AR-TAU1
10 μM
24 hours
Measure the stoichiometry of EPI-001 binding to AR-TAU1, showing 1:1 and 1:2 protein to drug binding
Protein Sci. 2025 Jan;34(1):e5254.
AR-TAU5
10 μM
24 hours
Measure the stoichiometry of EPI-001 binding to AR-TAU5, showing 1:1 protein to drug binding
Protein Sci. 2025 Jan;34(1):e5254.
EPI-001 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
LNCaP CRPC xenograft model
I.v.
50 mg/kg body weight
Every other day for a total of 7 doses
All EPI analogs significantly inhibited CRPC tumor growth, with EPI-002 and EPI-005 showing better antitumor activity.
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 <<
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 <<
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 <<
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 <<
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