Summary of Biologic Evaluation Data of Radiolabeled CA-IX Imaging Probes Shown in Figure 1
| Biodistribution | |||||||
| Compound | Binding affinity Ki (nM) | Tumor model | Tumor uptake (%ID/g) | Tumor-to-blood ratio | Tumor-to-muscle ratio | Imaging data | Reference |
| A | NA | NA | NA | NA | NA | NA | 16 |
| B | 58 | HT-29 | 0.13 at 0.5 h | 0.75 at 0.5 h | NA | NA | 19 |
| C | 59 | HT-29 | 0.2–0.1 at 0.5–4 h | 0.0 at 0.5–4 h | NA | NA | 18 |
| D | 66 | HT-29 | 0.5–0.1 at 0.5–4 h | 0.4–0.5 at 0.5–4 h | NA | NA | 18 |
| E | NA | HT-29 | ≤0.1 at 0.5–4 h | ≤1.0 at 0.5–4 h | NA | NA | 18 |
| F | NA | HT-29 | ≤0.2 at 0.5–4 h | 0.2–1.0 at 0.5–4 h | NA | NA | 18 |
| G | 0.9 (R = 3-NO2) | NA | NA | NA | NA | NA | 22 |
| 5.4 (R = 4-Ac) | NA | NA | NA | NA | NA | 22 | |
| 0.3 (R = 2-CN) | NA | NA | NA | NA | NA | 22 | |
| H | 45 | HT-29 | 0.83 at 1 h | <1.0 at 1 h | <1.0 at 1 h | NA | 21 |
| I | 124 | HT-29, U373 | <0.25 at 2–4 h | NA | NA | No tumor visualization | 39 |
| J | 9.0 | NA | NA | NA | NA | NA | 23 |
| K | 9.3 (R = Me) | HT-29 | 0.51 at 1 h | ∼1.0 at 1 h | ∼1.0 at 1 h | No tumor visualization | 20 |
| 9.6 (R = Ac) | HT-29 | 0.59 at 1 h | ∼1.0 at 1 h | ∼1.0 at 1 h | No tumor visualization | 20 | |
| 9.1 (R = Cl) | HT-29 | 0.98 at 1 h | ∼1.0 at 1 h | ∼1.0 at 1 h | No tumor visualization | 20 | |
| L | 5.2 | NA | NA | NA | NA | NA | 24 |
| M | 7.0 | NA | NA | NA | NA | NA | 24 |
| N | 70 | HT-29 | 1.16 at 1 h | <1.0 at 1 h | ∼1.0 at 1 h | No tumor visualization | 21 |
NA = not available.