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抑制剂/激活剂

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凋亡与自噬

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MDV3100 (Enzalutamide)

MDV3100 (Enzalutamide) 恩杂鲁胺; MDV3100

Enzalutamide是一种androgen-receptor (AR)拮抗剂，在 LNCaP细胞中IC50为36 nM。研究证明 Enzalutamide 可促进自噬。

货号：
TK0172
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	915087-33-1
生物活性	Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.
分子式	C21H16F4N4O2S
分子量	464.44
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : ≥ 50 mg/mL (107.66 mM) H2O : ≥ 0.1 mg/mL (0.22 mM)
体内研究	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.
体外研究	Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 does in a competition assay with 16β-[F]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.
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纯度及产品资料	98%

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