Table 3. RTK Inhibitor-Based Radiotracers for Eph Receptor Imaging.
target | lead compound skeleton | IC50 enzyme | IC50 cells | developed by | radiolabeling for imaging |
---|---|---|---|---|---|
EphB4 | benzodioxolylpyrimidine (compound 1) | n.d. | 90 ± 50 nM | Bardelle 201023 | Mamat 201224 (fluorine-18) |
EphB4 | indazolylpyrimidine (compound 20) | 1.3 nM | 9 nM | Bardelle 201023 | Ebert 201525 (carbon-11) |
Ebert 201525 (fluorine-18) | |||||
multi-Eph | xanthine (compound 66) | 1.6 (5) nM | n.d. | Lafleur 200926 | Pretze 202027 (fluorine-18) |