Table 1.
a Evaluation of radiolabling efficiency (%) of bifunctional ligand-trastuzumab conjugates with 90Y (RT, 0.25M NH4OAC, pH 5.5) using bITLC and cHPLC (parenthesis)
| Time | 3p-C-NETA-trastuzumab | 3p-C-DEPA-trastuzumab | C-DTPA-trastuzumab | C-DOTA-trastuzumab |
|---|---|---|---|---|
| 1 min | 91.6 ± 3.1 (86.2 ± 3.5) |
30.6 ± 1.9 (29.3 ± 2.2) |
98.4 ± 0.4 (90.1 ± 1.2) |
23.1 ± 7.7 (24.1 ± 6.6) |
| 5 min | 99.6 ± 0.2 (94.4 ± 0.2) |
58.6 ± 1.6 (50.3 ± 1.8) |
98.7 ± 0.7 (89.9 ± 1.3) |
43.0 ± 9.9 (39.8 ± 8.3) |
| 10 min | 99.6 ± 0.3 (94.9 ± 1.4) |
66.3 ± 10.4 (58.2 ± 6.8) |
98.6 ± 0.8 (89.5 ± 0.8) |
56.5 ± 12.5 (50.9 ± 13.3) |
| 20 min | 99.6 ± 0.5 (93.1 ± 1.1) |
67.9 ± 7.2 (58.3 ± 7.1) |
98.7 ± 0.4 (89.3 ± 0.8) |
67.4 ± 12.2 (60.1 ± 15.2) |
| 30 min | 99.9 ± 0.1 (93.6 ± 0.9) |
67.50 ± 7.5 (57.4 ± 7.3) |
98.9 ± 0.3 (90.3 ± 0.6) |
69.7 ± 10.8 (62.7 ± 12.4) |
| 60 min | 99.8 ± 0.1 (93.4 ± 0.5) |
67.4 ± 9.0 (56.9 ± 5.3) |
99.2 ± 0.4 (90.0 ± 0.5) |
71.7 ± 8.9 (63.4 ± 11.3) |
a
Radiolabeling efficiency (mean ± standard deviation %) was measured in triplicate (n = 3);
b
ITLC eluent (20mM EDTA/0.15M NH4OAc);
c
HPLC mobile phase (0.05M NaSO4/0.02M NaH2PO4/0.05% NaN3, pH 6.8 or PBS, pH 7.4).