Review Article
Insulin-Like Growth Factor System in Cancer: Novel Targeted Therapies
Table 5
Few examples of small molecule TKIs (tyrosine kinase inhibitors) directed against IGF receptors.
| Small molecule inhibitor | Mode of action | Effects | Reference |
| NVP-AEW541 NVP-AEW54 in combination with gemcitabine | Kinase inhibition | Antineoplastic, tumour regression and inhibition of metastasis | [216, 217] |
| Picropodophyllin (PPP) | Against autophosphorylation at the substrate level | Inhibition and downregulation of IGF-1R | [218ā221] |
| BMS-554417 | ATP-competitive, dual kinase inhibition | Antiproliferative activity | [222] |
| INSM-18 | Reversible ATP-competitive | Inhibitor of transcription (blocking also cdc2, survivin, and VEGF) | [223] |
| OSI-906 | Reversible ATP-competitive | Derived from compound-1, also known as PQIP | [223] |
| XL-228 (XL-2280) | ā | Inhibits bcr-abl, scr, and IGF-1R | [224] |
| BVP-51004 Biovitrum (Cyclolignan PPP) | Non-ATP-competitive | Causes IGF-1R downregulation, probably through the induction of ubiquitination. | [223] |
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