EPI-001


CAS No. : 227947-06-0

227947-06-0
Price and Availability of CAS No. : 227947-06-0
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5mg $55 In-stock
10mg $88 In-stock
25mg $160 In-stock
50mg $260 In-stock
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Cat. No. : HY-100348
M.Wt: 394.89
Formula: C21H27ClO5
Purity: >98 %
Solubility: DMSO : 33.33 mg/mL (84.40 mM; Need ultrasonic)
Introduction of 227947-06-0 :

EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. 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 is active against castration-resistant prostate cancer[1][2][3]. IC50 & Target: IC50: 6 μM (AR NTD)[1] In Vitro: EPI-001 (5-100 μM; 7 d) inhibits PCa/CRPC cell growth in a dose-dependent manner[2].
EPI-001 (50 μM) inhibits endogenous AR mRNA and protein expression in PCa and CRPC cell lines[2].
EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5[2]. In Vivo: EPI-00 (20 mg/kg; i.v. every 5 d for 25 d) inhibits the growth of tumors and has no general toxicity in vivo[1].
EPI-00 (50 mg/kg; i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth[1].

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