Table 2 Stability data for 68Ga, 44Sc and 177Lu complexes of AAZTA5 and AAZTA5-TOC against human serum, PBS buffer and EDTA and DTPA in PBS buffer in percent of stable complex at specific time points (% labelled compound compared to free activity found at given time point)
From: AAZTA5/AAZTA5-TOC: synthesis and radiochemical evaluation with 68Ga, 44Sc and 177Lu
68Ga | 44Sc | 177Lu | |||||||
|---|---|---|---|---|---|---|---|---|---|
time | AAZTA5 | AAZTA5-TOC | time | AAZTA5 | AAZTA5-TOC | time | AAZTA5 | AAZTA5-TOC | |
HS | 30 min | 93.0 ± 0.8 | 98.1 ± 0.2 | 1 h | 93.7 ± 0.9 | 95.1 ± 0.6 | 1 h | 99.8 ± 0.1 | 92.5 ± 1.9 |
1 h | 92.7 ± 1.3 | 96.9 ± 0.2 | 4 h | 94.3 ± 1.7 | 94.3 ± 0.8 | 2 h | 99.7 ± 0.1 | 92.3 ± 2.6 | |
2 h | 85.3 ± 3.4 | 95.0 ± 0.3 | 8 h | 93.2 ± 1.1 | 95.0 ± 1.1 | 24 h | 99.9 ± 0.1 | 91.5 ± 2.1 | |
24 h | 91.3 ± 1.8 | 93.8 ± 1.0 | 7 d | 82.5 ± 3.2 | 86.3 ± 3.2 | ||||
PBS | 30 min | 97.5 ± 1.0 | 99.1 ± 0.2 | 1 h | 95.3 ± 0.9 | 97.3 ± 0.5 | 1 h | 97.8 ± 0.5 | 92.0 ± 1.4 |
1 h | 88.7 ± 0.5 | 99.2 ± 0.1 | 4 h | 92.7 ± 1.3 | 98.5 ± 0.9 | 2 h | 98.6 ± 0.4 | 93.5 ± 1.3 | |
2 h | 78.5 ± 4.5 | 99.3 ± 0.1 | 8 h | 95.9 ± 1.2 | 96.7 ± 1.4 | 24 h | 99.1 ± 0.6 | 91.0 ± 2.2 | |
24 h | 96.0 ± 0.8 | 94.7 ± 1.6 | 7 d | 96.0 ± 0.8 | 93.1 ± 1.8 | ||||
EDTA | 30 min | 93.0 ± 0.2 | 98.9 ± 0.4 | 1 h | 93.7 ± 1.3 | 96.0 ± 0.4 | 1 h | 98.9 ± 0.2 | 95.7 ± 2.4 |
1 h | 50.3 ± 7.4 | 99.4 ± 0.2 | 4 h | 90.0 ± 3.2 | 97.6 ± 0.7 | 2 h | 97.9 ± 0.3 | 95.1 ± 2.6 | |
2 h | 49.5 ± 2.5 | 99.6 ± 0.1 | 8 h | 92.3 ± 2.1 | 96.9 ± 1.0 | 24 h | 79.2 ± 2.9 | 86.8 ± 2.6 | |
24 h | 91.9 ± 1.8 | 95.4 ± 2.1 | 7 d | 48.9 ± 1.5 | 77.5 ± 2.3 | ||||
DTPA | 30 min | 84.3 ± 0.9 | 97.8 ± 0.2 | 1 h | 94.3 ± 0.9 | 98.7 ± 0.3 | 1 h | 99.1 ± 0.2 | 98.9 ± 0.5 |
1 h | 78.0 ± 1.4 | 99.4 ± 0.1 | 4 h | 92.5 ± 0.5 | 98.9 ± 0.7 | 2 h | 99.1 ± 0.1 | 96.2 ± 3.2 | |
2 h | 45.7 ± 1.3 | 99.6 ± 0.3 | 8 h | 93.8 ± 1.2 | 96.9 ± 1.5 | 24 h | 80.4 ± 5.4 | 82.8 ± 4.7 | |
24 h | 93.4 ± 1.1 | 92.6 ± 3.2 | 7 d | 59.0 ± 14.3 | 72.9 ± 5.6 | ||||