Table 9. Inhibition and Degradation Activity of 9o against Select Kinasesa.
| kinase | kinase assay IC50, nM | degradation assay DC50, nM |
|---|---|---|
| ROS1 | 0.8 | 3.8 |
| ROS1 (G2101A) | 10.9 | ND |
| ROS1 (G2032R) | 161 | 13.2 |
| ROS1 (G2101C) | 83 | ND |
| ROS1 (L2086F) | 218 | 5.4 |
| ALK | 0.9 | 1.7 |
| FAK/PTK2 | 2.4 | 1.5 |
| FER | 3.1 | 17 |
| FLT3 | 3.5 | >1000 |
| CHEK2 | 3.6 | 187 |
| FES | 7.5 | 320 |
| ERBB4/HER4 | 27 | >1000 |
| PTK2B | 34 | ND |
| CLK1 | 35 | >1000 |
| CAMK2D | 39 | 264 |
| CHEK1 | 40 | ND |
| ERBB2 | 42 | 474 |
| INSRR | 45 | ND |
| NUAK1 | 47 | ND |
| CAMK2G | 48 | ND |
| LTK | 54 | >1000 |
| EGFR | 69 | 255 |
| BRK (PTK6) | 76 | ND |
| RET | 82 | 58 |
| C-MET | 95 | >1000 |
a
Data represent average of duplicate measurements. ND—not determined.