Table 1.
Full ex vivo biodistribution data of 89Zr-DFO-MPA1 over time (hours, h) in PRAME positive K562 and negative BLCL (A) and THP-1 (B) tumor bearing male NSG mice. Biodistribution in PRAME negative BLCL tumor bearing mice is displayed at 72 h (A). At 24 h in THP-1 (B) a group of mice (n = 4)were co-administered with unlabeled MPA1 to block uptake. Data is expressed as mean %IA/g (± one standard deviation)
| A. K562 | ||||||
|---|---|---|---|---|---|---|
| 4 h | 24 h | 48 h | 72 h | 72 h BLCL | 120 h | |
| Blood | 67.5 ± 16.5 | 26.0 ± 1.9 | 9.9 ± 5.6 | 5.7 ± 2.8 | 12.1 ± 6.4 | 1.5 ± 0.7 |
| Tumor | 13.4 ± 5.2 | 34.5 ± 5.5 | 28.5 ± 10.8 | 25.2 ± 6.3 | 13.4 ± 7.9 | 16.4 ± 4.5 |
| Heart | 19.8 ± 11.6 | 8.8 ± 0.6 | 6.5 ± 2.3 | 4.4 ± 1.0 | 5.0 ± 1.6 | 3.3 ± 0.5 |
| Lungs | 44.9 ± 15.2 | 20.8 ± 1.9 | 10.9 ± 2.9 | 7.0 ± 2.0 | 7.5 ± 3.2 | 4.4 ± 0.6 |
| Liver | 52.1 ± 15.9 | 40.8 ± 6.2 | 45.2 ± 8.7 | 45.8 ± 6.6 | 40.2 ± 5.1 | 48.8 ± 5.2 |
| Spleen | 51.4 ± 25.6 | 162.7 ± 33.4 | 917.4 ± 417.9 | 248.4 ± 78.5 | 40.0 ± 4.4 | 328.2 ± 39.9 |
| Stomach | 3.2 ± 1.6 | 6.3 ± 2.3 | 4.9 ± 0.5 | 3.5 ± 0.6 | 3.6 ± 2.0 | 2.1 ± 0.4 |
| Sm. Intestine | 5.7 ± 3.4 | 11.6 ± 1.8 | 12.9 ± 1.8 | 9.2 ± 1.5 | 11.1 ± 2.7 | 7.9 ± 2.0 |
| Lg. Intestine | 9.8 ± 4.1 | 8.3 ± 1.1 | 9.8 ± 1.9 | 7.0 ± 1.3 | 5.1 ± 1.0 | 4.3 ± 0.5 |
| Kidneys | 20.4 ± 8.6 | 11.8 ± 0.3 | 8.9 ± 1.2 | 7.8 ± 1.6 | 7.3 ± 1.7 | 6.4 ± 0.7 |
| Muscle | 2.5 ± 1.0 | 3.6 ± 1.4 | 4.7 ± 1.7 | 1.8 ± 0.5 | 2.3 ± 0.8 | 2.2 ± 0.6 |
| Bone | 12.1 ± 4.4 | 13.7 ± 1.9 | 28.2 ± 6.3 | 16.2 ± 4.9 | 11.5 ± 1.9 | 30.5 ± 2.0 |
| Tail | 13.2 ± 10.6 | 9.5 ± 4.0 | 9.4 ± 5.6 | 5.6 ± 1.4 | 5.9 ± 1.2 | 5.7 ± 1.0 |
| Testis | 10.5 ± 5.3 | 6.0 ± 0.6 | 5.4 ± 0.8 | 5.3 ± 0.3 | 5.9 ± 1.0 | 5.1 ± 0.3 |
| B. THP-1 | |||||
|---|---|---|---|---|---|
| Organ | 4 H | 24 H | 24 H Block | 48 H | 72 H |
| Blood | 59.4 ± 15.3 | 36.7 ± 17.2 | 26.4 ± 3.3 | 21.1 ± 7.8 | 21.5 ± 4.5 |
| Tumor | 5.0 ± 2.8 | 34.9 ± 16.9 | 4.5 ± 3.2 | 62.0 ± 20.1 | 32.7 ± 9.2 |
| Heart | 11.4 ± 3.8 | 8.9 ± 3.5 | 5.6 ± 1.1 | 4.7 ± 1.3 | 6.4 ± 1.8 |
| Lungs | 47.7 ± 20.1 | 21.9 ± 8.6 | 16.5 ± 1.8 | 13.1 ± 5.7 | 10.7 ± 3.3 |
| Liver | 28.7 ± 5.5 | 27.2 ± 11.1 | 16.2 ± 2.6 | 22.8 ± 5.3 | 32.3 ± 6.1 |
| Spleen | 23.8 ± 4.7 | 41.9 ± 13.8 | 10.4 ± 2.1 | 54.0 ± 24.5 | 70.3 ± 14.2 |
| Stomach | 2.5 ± 0.6 | 3.7 ± 1.1 | 1.7 ± 0.1 | 2.7 ± 0.4 | 4.2 ± 1.0 |
| Sm. Intestine | 5.1 ± 0.7 | 8.0 ± 2.2 | 2.6 ± 0.3 | 7.4 ± 1.5 | 10.7 ± 1.6 |
| Lg. Intestine | 5.3 ± 0.5 | 5.6 ± 1.3 | 2.5 ± 0.2 | 4.4 ± 1.1 | 6.0 ± 1.4 |
| Kidneys | 13.8 ± 2.8 | 10.9 ± 4.4 | 6.4 ± 0.7 | 7.5 ± 2.4 | 8.1 ± 1.1 |
| Muscle | 0.9 ± 0.2 | 2.1 ± 1.0 | 1.5 ± 0.4 | 1.5 ± 0.4 | 2.1 ± 1.0 |
| Bone | 9.4 ± 2.1 | 5.0 ± 6.4 | 5.5 ± 1.0 | 13.2 ± 6.1 | 23.7 ± 8.2 |
| Tail | 16.1 ± 10.2 | 5.2 ± 2.3 | 6.4 ± 3.7 | 6.1 ± 1.6 | 6.1 ± 3.1 |
| Testis | 6.0 ± 1.2 | 9.6 ± 5.8 | 3.2 ± 0.3 | 4.7 ± 0.8 | 5.6 ± 0.6 |