. Author manuscript; available in PMC: 2013 Aug 28.

Published in final edited form as: J Nucl Med. 2012 Sep 14;53(11):1670–1675. doi: 10.2967/jnumed.112.105007

Table 4.

In vitro kinase inhibitor activities expressed as IC₅₀ (nmol/L) values

	Sunitinib [nM]	Cabozantinib [nM]
VEGFR1/FLT		12.2
VEGFR2/KDR	4	0.035
VEGFR3/FLT-4		6.0
MET		1.8
PDGFR-beta	4, 10
RET	50	9.8
KIT	1-10, 13	4.6
FLT3	250, 50 (ITD)	14.4
TIE2		14.3
AXL		7
CSF-1R	50-100

Key: IC₅₀ is the concentration required for 50% target inhibition. KIT is stem cell factor receptor. RET is glial cell-line-derived neurotrophic factor receptor. FLT3 is Fms-like tyrosine kinase-3. All values are as reported in the respective investigator’s brochures. Please note that published literature has also reported in vitro inhibitory activity for sunitinib at VEGFR1 and VEGFR3.^15-17