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 7 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related VEGFR/PDGFR Products |
|---|
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Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells. Isolinderalactone suppressed the expression of B-cell lymphoma 2 (BCL-2), as well as of survivin and X-linked inhibitor of apoptosis protein (XIAP). |
| Oglufanide
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. |
| KLTWQELYQLKYKGI
KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. |
| Protein LMWP
Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. |
| CBO-P11
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. |
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