[111In]Bz-DTPA-hEGF: Preparation and In Vitro Characterization of a Potential Anti-Glioblastoma Targeting Agent

摘要: The overexpression of epidermal growth factor receptors, EGFR, in glioblastomas is well documented. Hence, the EGFR can be used as target structure for a specific targeting glioblastomas. Both radiolabeled anti-EGFR antibodies and natural ligand EGF are candidate agents targeting. However, EGF, which has rather low molecular weight (6 kDa), might have better tissue penetration properties through both normal tumors comparison with anti-EGF their fragments. aim this study was to prepare evaluate vitro an EGF-based antiglioma conjugate residualizing label. Human recombinant (hEGF) coupled isothiocyanate-benzyl-DTPA. purified from unreacted chelator using solid-phase extraction labeled (111)In. labeling yield 87% +/- 7%. label reasonably stable; transchelation (111)In serum proteins about 5% after incubation at 37 degrees C during 24 hours. obtained [(111)In]benzyl-DTPA-hEGF characterized expressing glioma cell line U343MGaCl2:6. binding affinity, internalization, retention were studied. had receptor radioactivity quickly internalized. intracellular interrupted 71% 1% 59% 1.5% 45 hours, respectively. dissociation constant estimated 2.0 nM. results indicate that potential glioblastoma cells, possibly locoregional injection.