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Vandetanib (Zactima) Chemical Structure
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Biological Activity
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively. In vitro, two cell lines (OZ and HuCCT1), both of which harboured KRAS mutation, were refractory to vandetanib, one cell line (TGBC24TKB) was somewhat resistant, and another cell line (TKKK) was sensitive. The most sensitive cell line (TKKK) had EGFR amplification. Vandetanib (25 mg /kg/ day) significantly prolonged the time to metastasis in an intravenous model of TKKK metastasis. [1][2]
References on Vandetanib (Zactima)
- [1] Br J Cancer. 2009 Apr 21;100(8):1257-66.
- [2] http://en.wikipedia.org/wiki/Vandetanib ;
Chemical Information
| Molecular Weight (WM): | 475.35 |
|---|---|
| Formula: | C22H24BrFN4O2 |
| CAS No.: | 443913-73-3 |
| Synonyms: |
ZD6474
|
| Dissolve in (25°C): | DMSO ≥4mg/mL |
| Water <1mg/mL | |
| Ethanol ≥3mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Receptor Tyrosine Kinase >> VEGFR >> VEGFR Inhibitors
Angiogenesis >> VEGFR >> VEGFR Inhibitors
Receptor Tyrosine Kinase >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Receptor Tyrosine Kinase >> c-RET >> c-RET Inhibitors
Apoptosis >> c-RET >> c-RET Inhibitors
Angiogenesis >> VEGFR >> VEGFR Inhibitors
Receptor Tyrosine Kinase >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Receptor Tyrosine Kinase >> c-RET >> c-RET Inhibitors
Apoptosis >> c-RET >> c-RET Inhibitors
Notes:
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Selleck's high quality products have been used in several published research findings, including the following:
Contrary Effects of the Receptor Tyrosine Kinase Inhibitor Vandetanib on Constitutive and Flow-Stimulated Nitric Oxide Elaboration in Humans
Inhibition of poxvirus spreading by the anti-tumor drug Gefitinib (IressaTM)
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Vandetanib reduced extracellular nitrite levels in endothelial cells. MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]), 50 ng/mL of vascular endothelial growth factor (VEGF) or matched vehicle (PBS; 0.5 hours), and L-arginine and soluble N-ethylmaleamide sensitive factor attachment protein (SNAP) added (1.5 hours). Vandetanib lowered nitrite levels in MS1 Ecs (*P0.0003). VEGF was used a positive control and increased nitrite levels (**P0.02). These findings indicate that vandetanib lowered endothelial cell NO levels. - Vandetanib reduced extracellular nitrite levels in endothelial cells. MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]), 50 ng/mL of vascular endothelial growth factor (VEGF) or matched vehicle (PBS; 0.5 hours), and L-arginine and soluble N-ethylmaleamide sensitive factor attachment protein (SNAP) added (1.5 hours). Vandetanib lowered nitrite levels in MS1 Ecs (*P0.0003). VEGF was used a positive control and increased nitrite levels (**P0.02). These findings indicate that vandetanib lowered endothelial cell NO levels.
Data from [hypertension 2011.July;58:85-92] Vandetanib (Zactima) purchased from Selleck
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Vandetanib reduced phosphorylation of Akt in endothelial cells (ECs). MS1 ECs were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]; 1 hour). Western blotting analysis showed that vandetanib decreased phosphorylation of Akt (S473) in MS1 ECs (*P0.01; n6 per group, studies done in triplicate). These findings show that vandetanib reduced Akt activity. - Vandetanib reduced phosphorylation of Akt in endothelial cells (ECs). MS1 ECs were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]; 1 hour). Western blotting analysis showed that vandetanib decreased phosphorylation of Akt (S473) in MS1 ECs (*P0.01; n6 per group, studies done in triplicate). These findings show that vandetanib reduced Akt activity.
Data from [hypertension 2011.July;58:85-92] Vandetanib (Zactima) purchased from Selleck
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Vandetanib increases membrane localization of endothelial NO synthase (eNOS). MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]). Western blotting analysis showed that vandetanib increases membrane localization of eNOS compared with control (*P0.04; n4 per group, studies done in triplicate). These findings show that vandetanib increased the membrane localization of eNOS compared with control.
Vandetanib increases membrane localization of endothelial NO synthase (eNOS). MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]). Western blotting analysis showed that vandetanib increases membrane localization of eNOS compared with control (*P0.04; n4 per group, studies done in triplicate). These findings show that vandetanib increased the membrane localization of eNOS compared with control.
Data from [hypertension 2011.July;58:85-92] Vandetanib (Zactima) purchased from Selleck
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Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Vandetanib for 24 hours.
Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Vandetanib for 24 hours.
Data independently produced by Dr. Zhang of Tianjin Medical University Vandetanib (Zactima) purchased from Selleck
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| Vandetanib reduced extracellular nitrite levels in endothelial cells. MS1 endothelial cells (ECs) were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]), 50 ng/mL of vascular endothelial growth factor (VEGF) or matched vehicle (PBS; 0.5 hours), and L-arginine and soluble N-ethylmaleamide sensitive factor attachment protein (SNAP) added (1.5 hours). Vandetanib lowered nitrite levels in MS1 Ecs (*P0.0003). VEGF was used a positive control and increased nitrite levels (**P0.02). These findings indicate that vandetanib lowered endothelial cell NO levels. |
Data from [hypertension 2011.July;58:85-92]
| Vandetanib reduced phosphorylation of Akt in endothelial cells (ECs). MS1 ECs were incubated with 1 mol/L of vandetanib or matched vehicle (dimethyl sulfoxide [DMSO]; 1 hour). Western blotting analysis showed that vandetanib decreased phosphorylation of Akt (S473) in MS1 ECs (*P0.01; n6 per group, studies done in triplicate). These findings show that vandetanib reduced Akt activity. |
Data from [hypertension 2011.July;58:85-92]
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