Scheme 1. Synthetic route of precursor for [64Cu]PSMA-617.
Figure 1. Chromatogram of [64Cu]PSMA-617. (A) It is a radio-TLC peak image of free Cu-64: Rf=1.0 (B) It is a radio-TLC peak image of [64Cu]PSMA-617: Rf=0.5
Figure 2. In vitro serum stability assay. (A) It is radio-TLC peak images of [64Cu] PSMA-617 after incubation in human serum, mouse serum and saline during 0, 4, 24, 48 h. (B) It is a graph of stability (%) of [64Cu]PSMA-617 after incubation in human serum, mouse serum and saline during 0, 4, 24, 48h.
Figure 3. PSMA mRNA or protein expression level of human prostate cancer cell line 22RV1, LNCaP, PC3 and PC3-M. (A) It is a RT-PCR band for PSMA mRNA expression. (B) It is a western blot band for PSMA protein expression. The GAPDH expression is used for control.
Figure 4. In vitro cell uptake assay. It is a time-dependent graph of [64Cu]PSMA-617 in human prostate cancer cell line PC3, 22RV1 and LNCap.
Figure 5. The biodistribution (%ID/g) of radioactivity in Balb/c (nu/nu) mice (n=4) after the injection of [64Cu]PSMA-617 at 2, 4, 6, 24, 48h. The tissue uptake at 2 h is highest and decreased via liver and kidney during 48 h.
Figure 6. The PET/CT imaging of 22RV1 prostate xenograft tumor model after injection [64Cu]PSMA-617. (A) It is a dynamic PET/CT image after 30-60 min of [64Cu]PSMA-617 injection in 22RV1 prostate xenograft tumor model. (B) It is a time-dependent graph of tumor to muscle uptake ratio. (C) It is a static PET/CT image of [64Cu]PSMA-617 injection in 22RV1 prostate xenograft tumor model at 24 h, 48 h.
Table 1. The biodistribution (%ID/g) of radioactivity in Balb/c (nu/nu) mice (n=4) after the injection of [64Cu]PSMA-617 at 2, 4, 6, 24, 48h.
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