Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ~6 μM and a selective PPAR-gamma modulator.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 43.00 | |
10 mg | In stock | $ 70.00 | |
25 mg | In stock | $ 143.00 | |
50 mg | In stock | $ 253.00 | |
100 mg | In stock | $ 378.00 | |
200 mg | In stock | $ 562.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 47.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 70 mg/mL (177.3 mM)
Ethanol: 70 mg/mL (177.3 mM)
You can also refer to dose conversion for different animals. More
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EPI-001 227947-06-0 Apoptosis DNA Damage/DNA Repair Endocrinology/Hormones Metabolism PPAR Androgen Receptor Androgen amino-terminal anti-tumor domain inhibit Peroxisome proliferator-activated receptors PPARγ EPI001 transactivation EPI 001 Receptor NTD Inhibitor inhibitor