产品
编 号：F233616
分子式：C19H16N6O4S
分子量：424.43
分子式：C19H16N6O4S
分子量：424.43
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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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: 186497-07-4
产品详情
生物活性：
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.
体内研究：
Zibotentan (10 mg/kg; intraperitoneal injection; daily; for 21 days) treatment significantly inhibits tumor growth in mice. And Zibotentan treatment increases E-cadherin expression.Animal Model:Female athymic (nu+/nu+) mice (4-6 week of age) injected with wild-type A2780 cells
Dosage:10 mg/kg
Administration:Intraperitoneal injection; daily ; for 21 days
Result:Showed significant inhibition in tumor growth in mice.
体外研究：
Zibotentan potently inhibits the binding of 125iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with apIC50 (concentration to inhibit 50% of binding) value of 22 nM.Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells.Zibotentan (ZD4054; 1 μM; 24 hours) treatment shows significant inhibition of cell proliferation in serum-starved HEY, OVCA 433, SKOV-3, and A-2780 cells.Zibotentan (ZD4054; 1 μM; 48 hours) treatment induces an increase in apoptotic cells. Zibotentan inhibits bcl-2 and activates caspase-3 and poly(ADP-ribose) polymerase proteins..Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells.Zibotentan treatment also results in a reduction of ETAR-driven angiogenesis and invasive mediators, such as vascular endothelial growth factor, cyclooxygenase-1/2, and matrix metalloproteinase (MMP).
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.
体内研究：
Zibotentan (10 mg/kg; intraperitoneal injection; daily; for 21 days) treatment significantly inhibits tumor growth in mice. And Zibotentan treatment increases E-cadherin expression.Animal Model:Female athymic (nu+/nu+) mice (4-6 week of age) injected with wild-type A2780 cells
Dosage:10 mg/kg
Administration:Intraperitoneal injection; daily ; for 21 days
Result:Showed significant inhibition in tumor growth in mice.
体外研究：
Zibotentan potently inhibits the binding of 125iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with apIC50 (concentration to inhibit 50% of binding) value of 22 nM.Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells.Zibotentan (ZD4054; 1 μM; 24 hours) treatment shows significant inhibition of cell proliferation in serum-starved HEY, OVCA 433, SKOV-3, and A-2780 cells.Zibotentan (ZD4054; 1 μM; 48 hours) treatment induces an increase in apoptotic cells. Zibotentan inhibits bcl-2 and activates caspase-3 and poly(ADP-ribose) polymerase proteins..Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells.Zibotentan treatment also results in a reduction of ETAR-driven angiogenesis and invasive mediators, such as vascular endothelial growth factor, cyclooxygenase-1/2, and matrix metalloproteinase (MMP).
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