Potency end-point :
IC50
c-Met 1.3 nM, Ret 4 nM, Kit 4.6 nM, Flt-1/3/4 12 nM/11.3 nM/6 nM, Tie2 14.3 nM, AXL 7 nM
Potency assay (off target):
AlphaScreen Assay, Coupled Luciferase Assay, Radiometric Assay
Probe Selectivity in
Vitro:
The inhibition profile of cabozantinib against a broad panel of 270 human kinases was determined using luciferase-coupled chemiluminescence 33P-phosphoryl transfer, or AlphaScreen technology. Cabozantinib is also a MET (Met Mutants) inhibitor with IC50s in the range of 1-15 nM.
