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EPI-001 is a specific inhibitor of the AR (androgen receptor) without inhibiting PR or GR transcriptional activities. EPI-001 selectively interacts with transactivation unit 5 (Tau-5) of the androgen receptor, which is essential for prostate cells to proliferate in the absence of androgens. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ.
EPI-001 (20 mg/kg; i.v. every 5 d for 25 d) inhibits the growth of tumors and has no general toxicity in vivo. EPI-001 (50 mg/kg; i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth.
EPI-001 is active against castration-resistant prostate cancer (CRPC) in xenografts.
| Molecular Weight | 394.89 |
| Formula | C21H27ClO5 |
| CAS Number | 227947-06-0 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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