Table 1. Chemical and Biological Characterization Data for 64Cu-DOTA-T/N- and 89Zr-DFO-T/N-trastuzumab Bioconjugates.
| radionuclide | chelator | initial Nor/mAb reaction stoichiometry | chelates/mAba | specific activity (mCi/mg) | immunoreactive fractionb | stabilityc |
|---|---|---|---|---|---|---|
| 64Cu | DOTA | 1.5 | 1.0 ± 0.2 | 3.2 ± 0.4 | 0.96 ± 0.05 | >98% |
| 3 | 2.3 ± 0.4 | 3.1 ± 0.2 | 0.95 ± 0.03 | >96% | ||
| 5 | 3.7 ± 0.7 | 5.3 ± 0.5 | 0.94 ± 0.02 | >96% | ||
| 89Zr | DFO | 1.5 | 1.1 ± 0.3 | 2.7 ± 0.2 | 0.96 ± 0.03 | >98% |
| 3 | 2.2 ± 0.3 | 2.9 ± 0.3 | 0.96 ± 0.04 | >98% | ||
| 5 | 3.8 ± 0.9 | 4.3 ± 0.4 | 0.93 ± 0.05 | >97% |
a
n = 3 for all experiments presented.
b
Determined prior to in vivo experimentation.
c
Calculated for incubation in human serum at 37 °C for 48 h (Cu) or 7 d (Zr).