产品
编 号：F087064
分子式：C25H32F3N7O2
分子量：519.56
分子式：C25H32F3N7O2
分子量：519.56
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1240299-33-5
产品详情
生物活性：
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer.
体内研究：
AZD3514 (10-100 mg/kg; p.o. once daily for 6 days) inhibits AR signaling in rats.AZD3514 (50 mg/kg; p.o. once daily for 30 days) inhibits prostate tumor growth.AZD3514 (50-100 mg/kg; p.o. once daily for 3 days) significantly reduces nuclear AR protein in vivo.Animal Model:Intact or castrat 42- and 49-day-old Hans Wistar rats
Dosage:10, 50 and 100 mg/kg
Administration:Oral gavage; 10-100 mg/kg once daily; for 6 days
Result:Inhibited AR signaling in rats, reduced seminal vesicle weight in intact rats, and inhibited the ability of exogenous testosterone proprionate to cause an increase in seminal vesicle weight in castrated rat.
Animal Model:Male Copenhagen rats with Dunning R3327H prostate tumors
Dosage:50 mg/kg
Administration:Oral gavage; 50 mg/kg once daily; for 30 days
Result:Significantly inhibited prostate tumor growth of rats.
体外研究：
AZD3514 (0-10 μM/L; 7 d) inhibits LNCaP and LAPC4 cells proliferation.AZD3514 (0-10 μM/L; 24 h) inhibits the ligand-driven expression of known AR-regulated genes.AZD3514 (0-30 μM/L; 24 h) reduces AR protein expression in LNCaPs and LAPC4s.AZD3514 (1-10 μM/L; 2 h) reduces AR nuclear translocation in LNCaP cells.
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer.
体内研究：
AZD3514 (10-100 mg/kg; p.o. once daily for 6 days) inhibits AR signaling in rats.AZD3514 (50 mg/kg; p.o. once daily for 30 days) inhibits prostate tumor growth.AZD3514 (50-100 mg/kg; p.o. once daily for 3 days) significantly reduces nuclear AR protein in vivo.Animal Model:Intact or castrat 42- and 49-day-old Hans Wistar rats
Dosage:10, 50 and 100 mg/kg
Administration:Oral gavage; 10-100 mg/kg once daily; for 6 days
Result:Inhibited AR signaling in rats, reduced seminal vesicle weight in intact rats, and inhibited the ability of exogenous testosterone proprionate to cause an increase in seminal vesicle weight in castrated rat.
Animal Model:Male Copenhagen rats with Dunning R3327H prostate tumors
Dosage:50 mg/kg
Administration:Oral gavage; 50 mg/kg once daily; for 30 days
Result:Significantly inhibited prostate tumor growth of rats.
体外研究：
AZD3514 (0-10 μM/L; 7 d) inhibits LNCaP and LAPC4 cells proliferation.AZD3514 (0-10 μM/L; 24 h) inhibits the ligand-driven expression of known AR-regulated genes.AZD3514 (0-30 μM/L; 24 h) reduces AR protein expression in LNCaPs and LAPC4s.AZD3514 (1-10 μM/L; 2 h) reduces AR nuclear translocation in LNCaP cells.
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