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Formula | C21H27ClO5 |
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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.) |
Description | 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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Targets |
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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] |
Cell Assay:[1] |
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Animal Study:[1] |
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Prebiotic stachyose inhibits PRDX5 activity and castration-resistant prostate cancer development [ Int J Biol Macromol, 2024, 278(Pt 3):134844] | PubMed: 39168191 |
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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.