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Enzalutamide

CAS No. : 915087-33-1

產(chǎn)品活性：Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.

研究領域：Vitamin D Related/Nuclear Receptor  |  Autophagy

作用靶點：Androgen Receptor  |  Autophagy

In Vitro: Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 does in a competition assay with 16β-[¹⁸F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide inhibits the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys).
Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex.

In Vivo: Enzalutamide (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.
Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg.

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