Table 1.
Optimization of reaction conditions for Df chelate conjugation and radiochemistry to prepare 89Zr-Df-Bz-rituximab.
| aDf-Bz chelate conjugation to antibody | ||||
|---|---|---|---|---|
| pH | Time (minutes) | Mab (nmoles) |
Df-bz Chelates (excess nm fold) |
Chelates/Mab (c/a) |
|
| ||||
| 8 | 45 | 0.5 | 5 | 1.30 ± 0.14 |
| 8 | 45 | 0.5 | 7.5 | 1.55 ± 0.07 |
| 8 | 45 | 0.5 | 10 | 2.20 ± 0.14 |
| 8.5 | 45 | 0.5 | 5 | 1.55 ± 0.07 |
| 8.5 | 45 | 0.5 | 7.5 | 2.30 ± 0.14 |
| 8.5 | 45 | 0.5 | 10 | 2.35 ± 0.07 |
| 9 | 45 | 0.5 | 5 | 1.65 ± 0.21 |
| 9 | 45 | 0.5 | 7.5 | 2.30 ± 0.14 |
| 9 | 45 | 0.5 | 10 | 2.60 ± 0.57 |
| b Radiochemical yield optimization | ||
|---|---|---|
| Radiochemical yield (%) | ||
|
| ||
| 6.5 | 45 | 74.06 ± 3.51 |
| 7 | 45 | 76.25 ± 0.86 |
| 7.5 | 45 | 76.49 ± 0 |
| 6.5 | 60 | 76.16 ± 1.05 |
| 7 | 60 | 77.01 ± 2.16 |
| 7.5 | 60 | 76.78 ± 1.24 |
Temperatures: a= 25° C; b= 37° C