Table 3 Potency of TKIs for inhibition of selected tyrosine kinase receptors

From: Changes in tumour vessel density upon treatment with anti-angiogenic agents: relationship with response and resistance to therapy

 

Sunitinib IC 50 ±s.e.m. (nM)

Pazopanib IC 50 (nM)

Cediranib IC 50 ±s.e.m. (nM)

Regorafenib IC 50 ±s.d. (nM)

VEGFR1

2

10

5±2

13±0.4

VEGFR2

9±2

30

<1

4.2±1.6

VEGFR3

17

47

≤3

46±10

PDGFRα

5–10

71

36±8

NA

PDGFRβ

8±3

84

5±1

22±3

c-kit

13

74

2±0.1

7±2

Flt3

1-10

NA

>1000

NA

TIE2

NA

4520

NA

311±46

FGFR1

830±120

140

26±9

202±18

  1. Abbreviations: IC50=mean inhibitory concentration 50; NA=data were not available; PDGFR=platelet-derived growth factor receptor; TKIs=tyrosine kinase inhibitors; VEGFR=vascular endothelial growth factor receptor.
  2. Table shows activity obtained within in vitro kinase assays and is based on the values reported in the following studies: sunitinib (Mendel et al, 2003; Cowey et al, 2010b), pazopanib (Kumar et al, 2007), cediranib (Wedge et al, 2005), regorafenib (Wilhelm et al, 2011).
  3. When available, data are quoted with s.d. or s.e.m.
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