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Enzalutamide

CAS No. : 915087-33-1

MCE 站：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。Enzalutamide 是一种自噬 (autophagy) 激活剂。

研究领域：Others  |  Autophagy

作用靶点：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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