Specificity and potency of CHIR-258 kinase inhibitor
Receptor tyrosine kinases . | CHIR-258 IC50, μM . |
|---|---|
| FLT3 | 0.001 |
| c-KIT | 0.002 |
| CSF-1R/c-fms | 0.036 |
| FGFR1 | 0.008 |
| FGFR3 | 0.009 |
| VEGFR1/Flt1 | 0.01 |
| VEGFR2/Flk1 | 0.013 |
| VEGFR3/Flt4 | 0.008 |
| PDGFRβ | 0.027 |
| PDGFRα | 0.21 |
| InsR | 2 |
| EGFR1 | 2 |
| c-Met | > 3 |
| EphA2 | 4 |
| Tie2 | 4 |
| IGFR1 | > 10 |
| HER2 | > 10 |
Receptor tyrosine kinases . | CHIR-258 IC50, μM . |
|---|---|
| FLT3 | 0.001 |
| c-KIT | 0.002 |
| CSF-1R/c-fms | 0.036 |
| FGFR1 | 0.008 |
| FGFR3 | 0.009 |
| VEGFR1/Flt1 | 0.01 |
| VEGFR2/Flk1 | 0.013 |
| VEGFR3/Flt4 | 0.008 |
| PDGFRβ | 0.027 |
| PDGFRα | 0.21 |
| InsR | 2 |
| EGFR1 | 2 |
| c-Met | > 3 |
| EphA2 | 4 |
| Tie2 | 4 |
| IGFR1 | > 10 |
| HER2 | > 10 |