2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  3. Androgen Receptor PPAR Apoptosis
  4. EPI-001

EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.

For research use only. We do not sell to patients.

EPI-001 Chemical Structure

EPI-001 Chemical Structure

CAS No. : 227947-06-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 60 In-stock
Solution
10 mM * 1 mL in DMSO USD 60 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 88 In-stock
25 mg USD 160 In-stock
50 mg USD 260 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of EPI-001:

EPI-001 Related Antibodies

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • Biological Activity

  • Purity & Documentation

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Description

EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer[1][2][3].

IC50 & Target

IC50: 6 μM (AR NTD)[1]
In Vitro

EPI-001 (5-100 μM; 7 d) inhibits PCa/CRPC cell growth in a dose-dependent manner[2].
EPI-001 (50 μM) inhibits endogenous AR mRNA and protein expression in PCa and CRPC cell lines[2].
EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EPI-001 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: PCa, CRPC, PC-3, DU 145, and T47D cell lines
Concentration: 0, 5, 10, 25, 50, 100 μM
Incubation Time: 7 days
Result: Inhibited growth of LNCaP cells at low concentrations.
Inhibited growth of AR-negative PC-3 and DU 145 cell lines as well as the T47D breast carcinoma cell line.

Western Blot Analysis[2]

Cell Line: LNCaP, VCaP LAPC4, C4-2,22Rv1, and CWR-R1 cells
Concentration: 50 μM
Incubation Time: 8-16 hours
Result: Decreased expression of full-length AR protein to varying degrees.
In Vivo

EPI-00 (20 mg/kg; i.v. every 5 d for 25 d) inhibits the growth of tumors and has no general toxicity in vivo[1].
EPI-00 (50 mg/kg; i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NOD-SCID mice (6-8 weeks) bearing LNCaP[1]
Dosage: 20 mg/kg
Administration: I.v. every 5 days for 25 days
Result: Reduced tumors from 100.3±1.72 mm3 to 73.03±29.6 mm3 within 2 weeks.
Did not cause general toxicity indicated by no change in animal behavior or body weight.
Molecular Weight

394.89

Formula

C21H27ClO5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (84.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5324 mL 12.6618 mL 25.3235 mL
5 mM 0.5065 mL 2.5324 mL 5.0647 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.87%

SDS (393 KB)

COA (243 KB) HNMR (270 KB) LCMS (261 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5324 mL 12.6618 mL 25.3235 mL 63.3088 mL
5 mM 0.5065 mL 2.5324 mL 5.0647 mL 12.6618 mL
10 mM 0.2532 mL 1.2662 mL 2.5324 mL 6.3309 mL
15 mM 0.1688 mL 0.8441 mL 1.6882 mL 4.2206 mL
20 mM 0.1266 mL 0.6331 mL 1.2662 mL 3.1654 mL
25 mM 0.1013 mL 0.5065 mL 1.0129 mL 2.5324 mL
30 mM 0.0844 mL 0.4221 mL 0.8441 mL 2.1103 mL
40 mM 0.0633 mL 0.3165 mL 0.6331 mL 1.5827 mL
50 mM 0.0506 mL 0.2532 mL 0.5065 mL 1.2662 mL
60 mM 0.0422 mL 0.2110 mL 0.4221 mL 1.0551 mL
80 mM 0.0317 mL 0.1583 mL 0.3165 mL 0.7914 mL
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EPI-001 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EPI-001227947-06-0EPI001EPI 001Androgen ReceptorPPARApoptosisPeroxisome proliferator-activated receptorsAndrogenReceptorARtransactivationamino-terminaldomainNTDPPARγanti-tumorInhibitorinhibitorinhibit

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