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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 | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
5 mg | $43 | In Stock | |
10 mg | $70 | In Stock | |
25 mg | $129 | In Stock | |
50 mg | $213 | In Stock | |
100 mg | $318 | In Stock | |
200 mg | $473 | In Stock | |
1 mL x 10 mM (in DMSO) | $47 | 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) |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 55 mg/mL (139.28 mM), Sonication is recommended. Ethanol: 70 mg/mL (177.3 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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