Table 1. CYC10268 potently and selectively inhibits kinase activity of CSF-1Ra
| Kinase |
Family |
CYC10268 |
Imatinib |
|
| CSF-1R |
Type III RTK |
0.015 |
0.033 |
| Kit |
Type III RTK |
0.21 |
0.066 |
| PDGF-R |
Type III RTK |
0.089 |
0.046 |
| KDR |
RTK |
>5 |
>5 |
| Insulin R |
RTK |
>5 |
>5 |
| Jak 1 |
Jak |
>5 |
>5 |
| Jak 2 |
Jak |
>5 |
>5 |
| Jak 3 |
Jak |
>5 |
>5 |
| Zap70 |
Syk/ZAP |
>5 |
>5 |
| Hck |
Src |
 5 |
>5 |
| Abl |
Abl |
>5 |
0.319 |
|
a In vitro kinase assays were performed on the kinase domains of a range of human kinases in the presence of CYC10268 or imatinib over a dose response from 0–5 µM. The IC50 values (µM) for CYC10268 and imatinib across the panel of kinases are displayed. In cases where the highest concentration of CYC10268 or imatinib did not inhibit kinase activity, IC50 is given as >5 µM.
