Skip to main content

Table 1 The IC50 values and targets of the approved kinase inhibitors against PDGFRs

From: PDGF/PDGFR effects in osteosarcoma and the “add-on” strategy

Kinase name Imatinib Dasatinib Nilotinib Sorafenib Sunitinib Pazopanib
IC50 values
 PDGFR-α [49] 2.5 2.6 2.4 1.0 13 20
 PDGFR-α [T674I] [50] 8500   4100 100 19 170
 PDGFR-α [V561D] [50] 9.1 2.9 15 5.6 14 21
 PDGFR-β [53] 68 1.1 60 34 5.7 42
Primary targets [53, 54] Abl, PDGFR, Kit Abl, Src Kit, Abl, PDGFR Raf, VEGFR, PDGFR, Kit, Flt3 PDGFR, VEGFR, Kit, Flt3 VEGFR, PDGFR, Kit
Secondary targets [53, 54] Raf PDGFR, Kit     FGFR
  1. Primary targets: The targets that are inhibited at the lowest concentrations (regardless of absolute concentrations)
  2. Secondary targets: The targets that are inhibited by about tenfold higher inhibitor concentrations