Article Figures & Data
Figures
- FIGURE 1.
(A) Chemical structures of TEFAPI-06 and TEFAPI-07. (B) Competition assays of TEFAPI-06 and TEFAPI-07. (C) Saturation binding assays of radiolabeled TEFAPI-06 and TEFAPI-07. (D) Cellular uptake assays of 68Ga-TEFAPI-06 and 68Ga-TEFAPI-07 in HT-1080-FAP and HT-1080 cells. IC50 = half-maximal inhibitory concentration.
- FIGURE 2.
(A) Dynamic PET imaging of 68Ga-TEFAPI-06 and 68Ga-TEFAPI-07 in healthy NOD/SCID mice. (B) Corresponding blood time–activity curves of 68Ga-TEFAPI-06 and 68Ga-TEFAPI-07.
- FIGURE 3.
(A) PET imaging of 86Y-TEFAPI-06 and 86Y-TEFAPI-07 in PDX-bearing mice. (B) Time–activity curves for tumor and major organs of 86Y-TEFAPI-06 and 86Y-TEFAPI-07.
- FIGURE 4.
(A) PET imaging of 86Y-TEFAPI-06 and 86Y-TEFAPI-07 in HT-1080-FAP and HT-1080 tumor–bearing mice at 24 h after injection. (B) Uptake of 86Y-TEFAPI-06 and 86Y-TEFAPI-07 in HT-1080-FAP and HT-1080 tumors at 24 h after injection. ***P < 0.001.
- FIGURE 5.
Biodistribution study of 177Lu-TEFAPI-06 and 177Lu-TEFAPI-07 in pancreatic cancer PDX–bearing mice at 96 h after injection (n = 5).
- FIGURE 6.
Treatment assay of 177Lu-TEFAPI-06 and 177Lu-TEFAPI-07 in pancreatic cancer PDX-bearing mice. (A) Design of therapy protocols and treatment scheme. (B) Tumor growth curve after treatment (n = 7–9 mice for each group). (C) Body weight change after treatment.
Tables
177Lu-TEFAPI-06 177Lu-TEFAPI-07 24 h 96 h 24 h 96 h Organ Mean SD Mean SD Mean SD Mean SD Blood 12.32 1.33 2.25 0.68 5.64 1.49 0.51 0.24 Pancreas 2.01 0.26 0.75 0.42 2.16 0.69 0.53 0.22 Spleen 3.00 0.66 3.66 1.22 2.69 0.87 1.88 0.34 Small intestine 2.55 0.64 0.61 0.28 1.19 0.26 0.16 0.09 Large intestine 1.66 0.27 0.53 0.35 1.15 0.33 0.10 0.15 Liver 2.98 0.64 1.74 0.57 3.21 0.81 2.31 0.17 Kidney 3.20 0.84 2.66 0.54 8.67 2.30 10.16 3.28 Stomach 1.75 0.17 0.54 0.21 1.20 0.45 0.29 0.14 Fat 1.86 0.90 1.55 1.17 1.82 1.18 0.48 0.25 Muscle 1.09 0.18 0.45 0.05 1.00 0.37 0.28 0.16 Bone 1.32 0.30 0.35 0.20 1.71 0.63 0.18 0.28 Lung 4.33 1.44 1.95 0.70 2.58 0.75 0.73 0.28 Heart 3.70 1.59 1.51 0.42 2.53 1.19 0.62 0.17 Brain 0.37 0.08 0.09 0.03 0.23 0.09 −0.01 0.04 Tumor 8.68 0.73 7.33 2.28 7.87 2.08 7.57 2.68 Data are %ID/g.
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