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Chemical Structure| 227947-06-0 Chemical Structure| 227947-06-0

Structure of EPI-001
CAS No.: 227947-06-0

Chemical Structure| 227947-06-0

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CAS No.: 227947-06-0

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EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ~6 μM and a selective PPAR-gamma modulator.

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Product Details of EPI-001

CAS No. :227947-06-0
Formula : C21H27ClO5
M.W : 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
InChI Key :HDTYUHNZRYZEEB-UHFFFAOYSA-N
Pubchem ID :4166922

Safety of EPI-001

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Androgen Receptor

    Androgen Receptor, IC50:~6 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
COS-1 cells 25 μM 24 hours EPI-001 effectively attenuated ARv567es variant activity. PMC3696543
WRL68 cells 25 μM 72 hours EPI-001 reduced lipid accumulation in hepatic cells PMC9785868
C4-2 cells 50 μM Inhibition of AR transcriptional activity PMC4414155
LNCaP cells 25 μM 48 hours To evaluate the effect of JNJ-64619178 on DNA damage repair, results showed JNJ-64619178 significantly inhibited DNA damage repair PMC3696543
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. PMC10098645
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). PMC10098645
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 PMC11635395
AR-TAU5 10 μM 24 hours Measure the stoichiometry of EPI-001 binding to AR-TAU5, showing 1:1 protein to drug binding PMC11635395
AR-AF1 4 μM 10 minutes Measure the stoichiometry of EPI-001 binding to AR-AF1, showing 1:1 and 1:2 protein to drug binding PMC11635395
LNCaP cells 50 μM To evaluate the effect of JNJ-64619178 on DNA damage repair, results showed JNJ-64619178 significantly inhibited DNA damage repair PMC4414155

In Vivo:

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. PMC3696543
Mice LNCaP xenograft model Intravenous injection 2 weeks EPI-001 significantly reduced the weight of benign prostates and caused regression of CRPC tumors PMC3132148
C57BL/6J mice HFHS diet-induced hepatic steatosis model Intraperitoneal injection 10 mg/kg or 30 mg/kg Every three days for 8 weeks EPI-001 ameliorated hepatic steatosis in mice PMC9785868

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01839760 - Completed - United States, Illinois ... More >> 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 Less <<
NCT02188004 - Completed - China, Guangxi ... More >> Liuzhou Center of disease prevention and control Liuzhou, Guangxi, China Less <<
NCT02645396 - Active, not recruiting December 2018 China, Fujian ... More >> Maternity and Child care of Huli District Xiamen, Fujian, China, 361000 China, Henan Maternity and Child care of Xinmi City Zhengzhou, Henan, China, 450000 Less <<
NCT01705964 Asthma Phase 4 Completed - United States, Kentucky ... More >> Kosair Children's Hospital Louisville, Kentucky, United States, 40202 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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