Table A2.
Inhibitory concentrations (IC50) in nmol for targets with multi-targeted tyrosine kinase inhibitors [303,304,305,306,307,308,309,310,311,312,313].
| VEGFR1 | VEGFR2 | VEGFR3 | PDFGRa | PDGFRb | c-KIT | RET | Flt-3 | MET | CSF-1R | FGFR1 | FGFR2 | FGFR2 | FGFR4 | Axl | |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sunitinib | 2 | 9 | 17 | 7 | 8 | 7 | 10 | 250 | - | 890 | 830 | - | - | - | 9 |
| Pazopanib | 10 | 30 | 47 | 71 | 81 | 74 | - | - | - | - | 140 | - | 130 | 80 | - |
| Tivozanib | 30 | 6 | 15 | 40 | 49 | 78 | - | 2550 | 550 | - | 525 | - | 1250 | 1400 | - |
| Axitinib | 0.1 | 0.2 | 0.1–0.3 | 5 | 1.6 | 1.7 | >1000 | >1000 | - | 73 | 100 | - | - | - | - |
| Cabozantinib | - | 0.035 | - | - | 234 | 4.6 | 5.2 | 11.3 | 1.3 | - | 5294 | - | - | - | 7 |
| Lenvatinib | 22 | 4 | 5.2 | 25 | 39 | 0.7 | 12 | - | 1900 | - | 46 | - | - | 43 | - |
| Sorafenib | 26 | 90 | 20 | - | 57 | 68 | - | 33 | - | - | 580 | - | - | - | - |
| Regorafenib | 13 | 4.2 | 46 | - | 22 | 7 | 1.5 | - | - | - | 202 | - | - | - | - |
| Nintedanib | 34 | 21 | 13 | 59 | 65 | - | - | 26 | - | - | 69 | 37 | 100 | 610 | - |
| Vandetanib | - | 40 | 110 | - | - | - | 100 | - | - | - | - | - | - | - | - |