Fig 1.
Chemical structures of NODAGA-JR11 and DOTA-TATE.
Fig 2.
Saturation binding of 64Cu-NODAGA-JR11 to HEK-hsst2 cells.
The cells were incubated with increasing concentrations of 64/natCu-NODAGA-JR11 (range 0.5–75 nM) for 2 hours at +4ºC.
Fig 3.
Saturation binding of 64/natCu-DOTA-TATE onto HEK-hsst2 cells.
The cells were incubated with increasing concentrations of 64Cu-DOTA-TATE (range 0.5–90 nM) for 2 hours at +4ºC.
Fig 4.
Internalization, binding, and dissociation of 64Cu-NODAGA-JR11.
HEK-hsst2 cells were incubated with 64Cu-NODAGA-JR11 at +4°C for 120 minutes and the temperature was shifted to 37°C by adding warm media (A) or media containing 50 pmol of NODAGA-JR11 (B). The amount of cell-bound, internalized, and dissociated activity was determined between 0 to 120 minutes after the temperature shift.
Fig 5.
Externalization kinetics of 64Cu-DOTA-TATE in HEK-hsst2 cells.
HEK-hsst2 cells were incubated with 64Cu-DOTA-TATE for 2 hours at +37°C. The receptor-bound ligands were removed by washing with glycine buffer, pH 2.8. Cells were then incubated by adding fresh medium and the amount of externalized and internalized (retained) radioactivity in the cells was measured after 10, 20, 30, 60, and 120 minutes.
Table 1.
Biodistribution of 10 pmol of 64Cu-NODAGA-JR11 in mice bearing HEK-hsst2 xenografts.
Table 2.
Biodistribution of 10 pmol of 64Cu-DOTA-TATE in mice bearing HEK-hsst2 xenografts.
Table 3.
Mass dependence of 64Cu-NODAGA-JR11 biodistribution in mice bearing HEK-hsst2 xenografts 1 hour p.i.
Fig 6.
PET images of 64Cu-NODAGA-JR11 distribution in HEK-hsst2 tumor-bearing mice.
Imaging data are presented as maximum intensity projections (MIP) at 1, 4, and 24 hours post-injection of 200 pmol of 64Cu-NODAGA-JR11.
Fig 7.
Mass dependence of the 64Cu-NODAGA-JR11 biodistribution in mice bearing HEK-hsst2 xenografts.
Imaging data are presented as MIP at 1 hour post-injection of 200, 1000, and 2000 pmol of 64Cu-NODAGA-JR11.