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Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase (IC50=40 nM). Vandetanib also inhibited VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM). Vandetanib had little effect on PDGFRβ, FLT-1, TIE-2 and FGFR1. IC50 was 1.1-3.6 μM, and had little effect on MEK, CDK2, C-kit, erbB2, FAK, PDK1, Akt and IGF-1R, with IC50 > 10 μM. Vandetanib inhibited the proliferation of HUVEC stimulated by VEGF-, EGF- and BFGF-with IC50 of 60 nM, 170 nM and 800 nM, respectively, but had little effect on the growth of basal endothelial cells. Vandetanib inhibits VEGFR-dependent tumor angiogenesis and EGFR - and RET - dependent tumor cell proliferation and survival to act on key signaling pathways in cancer. In transplanted tumor mice, Vandetanib inhibited the phosphorylation of VEGFR-2 and EGFR in tumor tissue, significantly reduced tumor vascular density, enhanced tumor cell apoptosis, inhibited tumor growth, improved survival rate, reduced the number of intrahepatic metastases, and upregulated VEGF, TGF-α, and EGF in tumor tissue. Vandetanib is currently being studied in phase III in patients with unresectable locally advanced or metastatic inherited or dispersed MTC.
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Vandetanib purchased from AbMole
| Molecular Weight | 475.35 |
| Formula | C22H24BrFN4O2 |
| CAS Number | 443913-73-3 |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
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| ABT-869
ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of VEGFR and PDGFR. |
| Tivozanib (AV-951)
Tivozanib (AV-951) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively. |
| Axitinib
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| Regorafenib
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Products are for research use only. Not for human use. We do not sell to patients.
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