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. Author manuscript; available in PMC: 2013 Feb 1.
Published in final edited form as: Curr Cancer Drug Targets. 2012 Feb;12(2):107–123. doi: 10.2174/156800912799095144

Table 1.

In vitro VEGFR, PDGFR, and FGFR kinase activity of multitargeted TKIs in clinical development for NSCLC.

Agent IC50, nM Other targets Clinical phase
VEGFR-1, -2, -3 PDGFR-α, -β FGFR-1, -2, -3
Sorafenib [77] NR, 90, 20a NR, 57a 580, NR, NR c-kit, FLT-3, Raf III
Sunitinib [78] NR, 80, NR NR, 2 2,900, NR, NR c-kit, FLT-3, CSF-1R, RET III
Cediranib [79] 5, 1, 3 36, 5 26, NR, NR c-kit III
Motesanib [80] 2, 3, 6 NR, 84 >2,800, NR, NR c-kit, RET III
Axitinib [81] NRb NRb NR c-kit II
Linifanib [82] 3, 4, 190 NR, 66 >12,500, NR, NR FLT-3, CSF-1R, c-kit II
Brivanib [83,84]c 380, 25, 10 NR, >6,000 148, 125, 68 NR II
BIBF 1120 [85] 34, 21, 13 59, 65 69, 37, 108 FLT-3, src III
Pazopanib [86] 10, 30, 47 71, 84 140, NR, 130 c-kit II/III
a

IC50 values of sorafenib against murine VEGFR-3 and PDGFR-β.

b

Axitinib reportedly inhibits VEGFRs at subnanomolar concentrations and PDGFR-β at low-nanomolar concentrations [81].

c

IC50 values for brivanib (BMS-582664) are reported for BMS-540215, the active moiety hydrolyzed in vivo.

c-kit, stem cell factor receptor; CSF-1R, colony stimulating factor 1 receptor; FGFR, fibroblast growth factor receptor; FLT-3, fms-like tyrosine kinase 3; IC50, half maximal inhibitory concentration; NR, not reported; PDGFR, platelet-derived growth factor receptor; Raf, v-raf 1 murine leukemia viral oncogene homolog 1; RET, rearranged during transfection; VEGFR, vascular endothelial growth factor receptor.