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Updated: May 27, 2026

Multi-photon Imaging of Tumor Cell Invasion in an Orthotopic Mouse Model of Oral Squamous Cell Carcinoma
Published on: July 25, 2011
PET imaging of EGF receptors using [18F]FBEM-EGF in a head and neck squamous cell carcinoma model
Weihua Li1, Gang Niu, Lixin Lang
1Department of Medical Imaging and Nuclear Medicine, Fourth Affiliated Hospital, Harbin Medical University, 37 Yinhang Street, Nangang District, Harbin 150001, China.
Purpose:
To prepare and evaluate a new radiotracer for molecular imaging of cell surface receptors for epidermal growth factor (EGF).
Methods:
Cys-tagged EGF (cEGF) was labeled with (18)F by coupling the free thiol group of the Cys tag with N-[2-(4-[(18)F]fluorobenzamido)ethyl]maleimide ([(18)F]FBEM) to form [(18)F]FBEM-cEGF. Cell uptake, internalization and efflux of [(18)F]FBEM-cEGF were tested in human head and neck squamous carcinoma UM-SCC1 cells. In vivo tumor targeting and pharmacokinetics of the radiotracers were evaluated in UM-SCC1 tumor-bearing athymic nude mice by static and dynamic microPET imaging. Ex vivo biodistribution assays were performed to confirm the noninvasive imaging results.
Results:
The radiolabeling yield for [(18)F]FBEM-cEGF was over 60%, based on starting [(18)F]FBEM. [(18)F]FBEM-cEGF exhibited rapid blood clearance through both hepatobiliary and renal excretion. UM-SCC1 tumors were clearly visualized and showed modest tracer uptake of 2.60 ± 0.59 %ID/g at 30 min after injection. Significantly higher tumor uptake of [(18)F]FBEM-cEGF (5.99 ± 1.61%ID/g at 30 min after injection, p < 0.01) and tumor/nontumor ratio were achieved by coinjection of 50 microg of unlabeled EGF. Decreased liver uptake of [(18)F]FBEM-cEGF was observed when unlabeled EGF was coadministered.
Conclusion:
With optimized liver blocking, [(18)F]FBEM-cEGF has the potential to be used in a noninvasive and quantitative manner for detection of malignant lesions and evaluation of EGFR activity.
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