Table 2.
a Evaluation of Radiolabling efficiency (%) of bifunctional ligand-trastuzumab conjugates with 177Lu (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 | 99.2 ± 0.2 (96.5 ± 1.2) |
35.9 ± 1.8 (29.8 ± 2.1) |
99.5 ± 0.3 (98.3 ± 0.6) |
29.7 ± 1.5 (28.1 ± 3.0) |
| 5 min | 99.9 ± 0.1 (97.7 ± 0.8) |
71.1 ± 2.2 (60.0 ± 1.9) |
99.4 ± 0.2 (98.3 ± 0.3) |
58.6 ± 1.3 (54.6 ± 1.5) |
| 10 min | 99.8 ± 0.1 (97.6 ± 1.3) |
85.3 ± 1.1 (75.2 ± 0.4) |
99.4 ± 0.4 (98.4 ± 0.7) |
75.5 ± 1.7 (70.1 ± 1.6) |
| 20 min | 99.9 ± 0.1 (97.6 ± 0.8) |
94.8 ± 0.4 (85.4 ± 1.0) |
99.6 ± 0.1 (98.3 ± 0.3) |
89.3 ± 0.1 (84.6 ± 1.4) |
| 30 min | 99.8 ± 0.1 (97.5 ± 0.3) |
97.9 ± 0.4 (87.3 ± 1.4) |
99.6 ± 0.2 (98.3 ± 0.3) |
94.2 ± 0.4 (90.1 ± 1.5) |
| 60 min | 99.9 ± 0.1 (97.4 ± 0.4) |
98.4 ± 0.8 (87.6 ± 1.3) |
99.4 ± 0.3 (98.1 ± 0.3) |
97.8 ± 0.3 (94.8 ± 1.3) |
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).