Table 1. IC50 values of Foretinib, Foretinib-TCO (11), and Foretinib-BODIPY-FL (12) for the indicated recombinant human kinases.
Compound | MET | AXL | RON | PDGFRα | KDR |
---|---|---|---|---|---|
Foretinib | 28.7 | 21.4 | 20.2 | 59.2 | 24.3 |
Foretinib-TCO | 88.6 | 72.5 | 82.7 | 264.6 | 149.9 |
Foretinib-BODIPY-FL | 697.4 | ND | ND | ND | ND |
Fold Change (TCO/Foretinib) | 3.1 | 3.4 | 4.1 | 4.5 | 6.2 |
All IC50 values are in nM and R2 values for the dose-response curve fit (GraphPad, Prism) were 0.92 or greater. Fold change is Foretinib-TCO (11) IC50 value divided by Foretinib IC50 value. ND: not determined.