Estimated IC50 values (nM) for selected kinases for cabozantinib and metabolites N.D. EXEL-1646, EXEL-5162, EXEL-5366, and EXEL-1644
| Kinase | Cabozantinib | EXEL-1646 | EXEL-5162 | EXEL-5366 | EXEL-1644 |
|---|---|---|---|---|---|
| Aurora-A | 381 | 152 | N.D. | N.D. | 1000 |
| Aurora-B | 23 | 52 | >3600 | >3600 | >1000 |
| AXL | 8 | 87 | N.D. | N.D. | >1000 |
| KIT | 752 | >1000 | >3600 | >3600 | >1000 |
| EGFR | >1000 | >1000 | >3600 | >3600 | >1000 |
| FLT1 | 13 | >1000 | >3600 | >3600 | >1000 |
| FLT3 | 21 | 155 | 530 | >3600 | >1000 |
| FLT4 | 3 | 175 | N.D. | N.D. | >1000 |
| KDR | 14 | 308 | 140 | >10000 | >1000 |
| MET | 2 | 199 | 190 | 5000 | >1000 |
| PDGFR N.D.β | 575 | >1000 | >3600 | >3600 | >1000 |
| RET | 8 | 234 | >1000 | >1000 | >1000 |
| RON | 46 | >1000 | N.D. | N.D. | <1000a |
| TIE2 | 13 | 60 | N.D. | N.D. | >1000 |
N.D., not determined.
↵a Residual activity 25% at 1 µM.