FIGURE 1.
(A) Binding of radiolabeled FAPI-01 and FAPI-02 to the 4 human cancer cell lines and to the HT-1080-FAP, HEK-muFAP, and HEK-CD26 cell lines after 60 min of incubation. (B) Internalization of radiolabeled FAPI-01 and FAPI-02 into HT-1080-FAP cells after incubation for 10 min to 24 h. Internalized fraction is gray or black, and extracellularly bound fraction is white. (C) Competitive binding of radiolabeled FAPI-01 and FAPI-02 to HT-1080-FAP cells after adding increasing concentrations of unlabeled FAPI-01 and Lu-FAPI-02. (D) Efflux kinetics of FAPI-01 and FAPI-02 after 1 h of incubation of HT-1080-FAP cells with radiolabeled compounds, followed by incubation with compound-free medium for 1–24 h. All data are %ID normalized to 1 million (mio) cells.