Summary of kinase inhibitory activities of ABT-869
| Kinase . | IC50, nM . |
|---|---|
| Structurally related RTKs* | |
| KDR | 4 |
| Flt1 | 3 |
| Flt4 | 190 |
| PDGFR-β | 66 |
| CSF-1R | 3 |
| KIT | 14 |
| Flt3 | 4 |
| TIE2 | 179 |
| RET | 1 900 |
| FGFR | > 12 500 |
| Nonrelated TKs* | |
| SRC | > 50 000 |
| IGFR | > 50 000 |
| INSR | > 50 000 |
| LCK | 38 000 |
| EGFR | > 50 000 |
| HCK | > 50 000 |
| CMET | > 50 000 |
| LYN | > 20 000 |
| FYN | > 50 000 |
| FGF | > 50 000 |
| Ser/Thr kinases† | |
| AKT | > 50 000 |
| SGK | 940 |
| CDC2 | 9 800 |
| PKA | 5 900 |
| Kinase . | IC50, nM . |
|---|---|
| Structurally related RTKs* | |
| KDR | 4 |
| Flt1 | 3 |
| Flt4 | 190 |
| PDGFR-β | 66 |
| CSF-1R | 3 |
| KIT | 14 |
| Flt3 | 4 |
| TIE2 | 179 |
| RET | 1 900 |
| FGFR | > 12 500 |
| Nonrelated TKs* | |
| SRC | > 50 000 |
| IGFR | > 50 000 |
| INSR | > 50 000 |
| LCK | 38 000 |
| EGFR | > 50 000 |
| HCK | > 50 000 |
| CMET | > 50 000 |
| LYN | > 20 000 |
| FYN | > 50 000 |
| FGF | > 50 000 |
| Ser/Thr kinases† | |
| AKT | > 50 000 |
| SGK | 940 |
| CDC2 | 9 800 |
| PKA | 5 900 |
Methods and data can be found in Albert et al.15
*IC50 values determined at an ATP concentration of 1 mM.
†IC50 values determined at an ATP concentration of 5 to 10 μM.