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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $43 | In Stock | In Stock | |
| 10 mg | $70 | In Stock | In Stock | |
| 25 mg | $129 | In Stock | In Stock | |
| 50 mg | $213 | In Stock | In Stock | |
| 100 mg | $318 | - | In Stock | |
| 200 mg | $473 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $47 | In Stock | In Stock |
| Description | EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ~6 μM and a selective PPAR-gamma modulator. |
| Targets&IC50 | Androgen receptor: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] |
| Cell Research | 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).(Only for Reference) |
| Synonyms | EPI001, EPI 001 |
| Molecular Weight | 394.89 |
| Formula | C21H27ClO5 |
| Cas No. | 227947-06-0 |
| Smiles | CC(C)(c1ccc(OCC(O)CO)cc1)c1ccc(OCC(O)CCl)cc1 |
| Relative Density. | 1.228 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 55 mg/mL (139.28 mM), Sonication is recommended. Ethanol: 70 mg/mL (177.26 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.06 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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