Table 5: Few examples of small molecule TKIs (tyrosine kinase inhibitors) directed against IGF receptors.

Small molecule inhibitorMode of actionEffectsReference

NVP-AEW54 in combination with gemcitabine
Kinase inhibitionAntineoplastic, tumour regression and inhibition of metastasis[216, 217]

Picropodophyllin (PPP)Against autophosphorylation at the substrate level Inhibition and downregulation of IGF-1R[218221]

BMS-554417ATP-competitive, dual kinase inhibitionAntiproliferative activity[222]

INSM-18 Reversible
Inhibitor of transcription (blocking also cdc2, survivin, and VEGF)[223]

Derived from compound-1, also known as PQIP[223]

XL-228 (XL-2280)Inhibits bcr-abl, scr, and IGF-1R[224]

BVP-51004 Biovitrum (Cyclolignan PPP)Non-ATP-competitiveCauses IGF-1R downregulation, probably through the induction of ubiquitination.[223]