Table 2. Binding Affinities Toward the Integrins αvβ6, αvβ8, α5β1, αvβ3, αvβ5, and αIIbβ3, Determined for the Nonradioactive Metal Complexes, Expressed as IC50 ± SD [nM].
| compound | αvβ6 | αvβ8 | α5β1 | αvβ3 | αvβ5 | αIIbβ3 |
|---|---|---|---|---|---|---|
| natLu-c(avb6)-Trz-DOTPI | 0.6 ± 0.1 | 116 ± 14 | 238 ± 59 | >1000 | >1000 | >1000 |
| natLu-c(avb6)-Trz-DOTAGA | 0.8 ± 0.2 | 113 ± 23 | 327 ± 3 | >1000 | >1000 | >1000 |
| natLu-c(avb6)-Trz-DOTA | 0.8 ± 0.1 | 158 ± 22 | 271 ± 83 | >1000 | >1000 | >1000 |
| natLu-c(avb6)-DOTAGA | 0.7 ± 0.1 | 123 ± 8 | 407 ± 96 | >1000 | >1000 | >1000 |
| natLu-c(avb6)-DOTA | 0.47 ± 0.03 | 43 ± 7 | 248 ± 24 | >1000 | >1000 | >1000 |
| natGa-c(avb6)-Trz-DOTAGA | 0.4 ± 0.2 | n.d. | n.d. | n.d. | n.d. | n.d. |
| natGa-c(avb6)-Trz-DOTA | 0.8 ± 0.3 | n.d. | n.d. | n.d. | n.d. | n.d. |
| natGa-c(avb6)-DOTAGA | 0.6 ± 0.1 | n.d. | n.d. | n.d. | n.d. | n.d. |
| natGa-c(avb6)-DOTA | 0.3 ± 0.03 | n.d. | n.d. | n.d. | n.d. | n.d. |
| natGa-c(avb6)-Ahx-NOPO | 1.98 ± 0.09 | 135 ± 26 | 440 ± 31 | >1000 | >1000 | >1000 |
| natGa-avebehexin18 | 0.26 ± 0.02 | n.d. | n.d. | n.d. | n.d. | n.d. |