Off target protein and potency: c-Met 1.3 nMRet 4 nMKit 4.6 nMFlt-1/3/4 12 nM/11.3 nM/6 nMTie2 14.3 nMAXL 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.