EPI-001

Catalog No.S7955 Batch:S795501

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Technical Data

Formula

C21H27ClO5
Molecular Weight 394.89 CAS No. 227947-06-0
Solubility (25°C)* In vitro DMSO 79 mg/mL (200.05 mM)
Ethanol 79 mg/mL (200.05 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Targets
PPARγ [2] Androgen Receptor [1]
(in LNCaP cells)
~6 μM
In vitro EPI-001 blocks transactivation of the AR NTD, interacts with the AF-1 region, inhibits protein-protein interactions with AR, and reduces AR interaction with androgen-response elements on target genes. In LNCaP cells, EPI-001 inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. [1] In LNCaP cells, EPI-001 also acts as a PPAR-gamma modulator to result in inhibition of androgen receptor expression and activity, which inhibits prostate cancer growth. [2]
In vivo In male mice bearing CRPC LNCaP s.c. xenografts, EPI-001 (50 mg/kg, i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth by reducing proliferation and increasing apoptosis. [1]

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    LNCaP cells

  • Concentrations

    10 μg/mL

  • Incubation Time

    4 days

  • Method

    LNCaP cells are treated with bicalutamide (BIC) or EPI-001 for 1 hr before the addition of R1881 (0.1 nM) for 4 days. LNCaP cells are treated with OCM (50%) with, or without, EPI-001 for 3 days (serum-free, androgen-free, phenol red-free conditions).
Animal Study:[1]
  • Animal Models

    Male mice bearing LNCaP s.c. xenografts

  • Dosages

    50 mg/kg

  • Administration

    i.v.

Selleck's EPI-001 has been cited by 6 publications

Rational optimization of a transcription factor activation domain inhibitor [ Nat Struct Mol Biol, 2023, 30(12):1958-1969] PubMed: 38049566
Effects of Oncolytic Vaccinia Viruses Harboring Different Marine Lectins on Hepatocellular Carcinoma Cells [ Int J Mol Sci, 2023, 24(4)3823] PubMed: 36835232
N-glycosylation of GDF15 abolishes its inhibitory effect on EGFR in AR inhibitor-resistant prostate cancer cells [ Cell Death Dis, 2022, 13(7):626] PubMed: 35853851
Oncolytic Vaccinia Virus Harboring Aphrocallistes vastus Lectin Inhibits the Growth of Hepatocellular Carcinoma Cells [ Mar Drugs, 2022, 20(6)378] PubMed: 35736181
Hybrid Androgen Receptor Inhibitors Outperform Enzalutamide and EPI-001 in in vitro Models of Prostate Cancer Drug Resistance [ ChemMedChem, 2022, e202200548.] PubMed: 36300876
Combined N-terminal androgen receptor and autophagy inhibition increases the antitumor effect in enzalutamide sensitive and enzalutamide resistant prostate cancer cells [ Prostate, 2019, 79(2):206-214] PubMed: 30345525

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.