Table 1.
Characteristics of PDGF receptor kinase inhibitors
Inhibitor | Primary targets | Secondary targets |
---|---|---|
Imatinib |
Abl, PDGFR, Kit |
Raf |
Sunitinib |
PDGFR, VEGFR, Kit, Flt3 |
|
Sorafenib |
Raf, VEGFR, PDGFR, Kit, Flt3 |
FGFR |
Pazopanib |
VEGFR, PDGFR, Kit |
FGFR |
Nilotinib |
Kit, Abl, PDGFR |
|
Cediranib |
VEGFR, Kit, PDGFR |
FGFR |
Motesanib |
VEGFR, Kit |
PDGFR, Ret |
Axitinib |
VEGFR |
PDGFR, Kit |
Linifenib |
VEGFR, Kit |
PDGFR |
Dasatinib |
Abl, Src |
PDGFR, Kit |
Quizartinib |
FLT3 |
Kit, PDGFR, Ret, CSF1R |
Ponatinib | Ret, Abl | PDGFR, VEGFR |
The table summarizes the specificities of some kinase inhibitors targeting PDGF receptors. The Kd:s of the different members of the PDGFR, VEGFR and FGFR families are often similar and are lumped together, for simplicity. As primary targets are listed the kinases that are inhibited at the lowest concentrations (regardless of absolute concentrations). As secondary targets are listed kinases that are inhibited by about 10-fold higher inhibitor concentrations. For references, see [3,50-54].