交易须知
enzalutamide产品活性：enzalutamide (mdv3100) 是一种雄激素受体 (androgen receptor (ar)) 拮抗剂，在lncap前列腺细胞中抑制ar 的 ic50 值为36 nm。
研究领域：others  |  autophagy
作用靶点：androgen receptor  |  autophagy
in vitro: enzalutamide has greater affinity to ar than bicalutamide 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 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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