Table 6.

Overview of tumor uptake and IC₅₀ values of isotopologue labelled clinically approved TKI drugs.

	U87	A549	H3255	PC9/PC14	HCC827	H1975	Other:
[18F]Gefitinib	Ex vivo:	ND	Ex vivo:	ND	ND	Ex vivo:	Ex vivo:
	SUV 0.14 ± 0.05		SUV 0.22 ± 0.09			SUV 0.15 ± 0.10	U87-EGFR
	at 120 min [84]		at 120 min [84]			at 120 min [84]	SUV 0.14 ± 0.06 at 120 min [84]
							Fibrosarcoma:
							3.5%ID/g at 60 min [83]
[11C]Erlotinib		Ex vivo:			Ex vivo:		Ex vivo:
		1.62 ± 0.47%ID/g			3.66 ± 0.14%ID/g		NCI358: 0.69 ± 0.11%ID/g at 60 min [95]
		at 60 min [95]			at 60 min [95]
	In vivo:	In vivo:	In vivo:	In vivo:	In vivo:	In vivo:	In vivo:
	SUV 0.51 ± 0.56	T/NT 1.0 ± 0.3	SUV 0.43 ± 0.01 at 12 min [97]	SUV 0.45 ± 0.31 at 90 min [94]	SUV 0.91 ± 0.60 at 90 min [94]	SUV 0.33 ± 0.03	SW620 (n = 1): SUV of 0.28 [94]
	at 90 min [94]	at 60–90 min [96]	SUV 0.33 ± 0.09 at 60 min [97]		SUV 0.60 ± 0.01 at 12 min [97]	at 12 min [97]	U87ΔEGFRvIII: SUV of 0.46 ± 0.29 [94]
					SUV 0.71 ± 0.07 at 60 min [97]	SUV 0.21 ± 0.03
					3.2 ± 0.3%ID/g at 25 min [96]	at 60 min [97]	QG56: SUV 0.34 ± 0.04 at 12 min [97]
					T/NT 1.9 ± 0.5 at 60–90 min [96]	T/NT 1.0 ± 0.3 at 60–90 min [96]	SUV 0.20 ± 0.01 at 60 min [97] IC50: 8.9 µM [97]
					VT 0.96 ± 0.15 in 10–60 min interval [88]		A431: VT 0.75 ± 0.06 in 10–60 min [88]
			IC50: 40nM [97]		IC50: 28.5 ± 4.5nM [88]	IC50: 4.3 µM [97]	HCC827ERLO: VT 1.05 ± 0.26 in 10–60 min, IC50: 9.8 ± 7.4µM
					IC50: 4 nM [97]		HCC827EPR: VT 1.00 ± 0.15 in 10–60 min, IC50: 5.4 ± 2.3µM [88]
[18F]Afatinib	ND	Ex vivo:	ND	ND	Ex vivo:		ND
		2.17 %ID/g at 5 min,			1.56 %ID/g at 5 min,
		T/M 6.37 at 120 min			T/M 3.83 at 120 min
		[91]			[91]
		In vivo:			In vivo:	In vivo:
		T/NT 1.5 ± 0.3			T/NT 2.3 ± 0.4	T/NT 0.8 ± 0.2
		at 90–120 min [96]			at 90–120 min [96]	at 90–120 min [96]
					1.2 ± 0.2%ID/g at 10 min [96]