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.