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[18F]4 is a fluorine-18 labeled small-molecule radioligand targeting vascular endothelial growth factor receptor-3 (VEGFR-3). Designed as a fluorinated analog of the VEGFR-3 inhibitor SAR131675, it was developed by Nemours Children's Health for positron emission tomography (PET) imaging of tumor lymphatic activity and lymphangiogenesis. In vitro characterization shows that the (R)-enantiomer of the compound exhibits high binding affinity for VEGFR-3 and moderate-to-high selectivity over VEGFR-1 and VEGFR-2. Preliminary preclinical PET imaging in healthy mice demonstrates high uptake in the liver, intestine, and gallbladder, with low uptake in the brain.
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