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. 2021 Sep 22;12(3):1363–1376. doi: 10.1016/j.apsb.2021.09.016

Figure 3.

Figure 3

Target engagement study of [64Cu]DPA in tumor models. (A) Fluorescence images of B6F10 cells after co-incubation with 5 μmol/L of FITC-DPA for 1 h at 37 °C. BF: bright field. Scale bar: 100 μm. (B) B16F10 cell uptake of radioactivity when incubation with [64Cu]DPA (20 μCi/mL), [64Cu]DPA (20 μCi/mL) + 1 mmol/L DPA, [64Cu]DPA (20 μCi/mL) + 1 mmol/L anti-PD-L1 for different incubation times. (C) Competitive binding of [64Cu]DPA (20 μCi/mL) to B16F10 cells co-incubated with different concentrations of either DPA or anti-PD-L1 for 120 min at 37 °C. The corresponding Ki values are also shown. (D) and (E) Co-registered PET/CT maximum intensity projection (MIP) images of C57BL/6J mice bearing big B16F10 tumors (D) and small B16F10 tumors (E) after intravenous injection of approximately 0.5 mCi of [64Cu]DPA for 30, 60, and 90 min. The white dashed circles indicate the tumors. (F)‒(H) PET image-derived time–activity curves (0–80 min) of B16F10 tumor (F), heart (G), and kidney (H) in C57BL/6J mice bearing B16F10 tumors after intravenous injection of [64Cu]DPA. Groups 1 and 2 correspond to mice shown in panels D and E. Data represent mean ± SD, n = 3.