Linsitinib

  • Chemical Properties
CAS No. 867160-71-2 Cat. No. BCP01831
Name Linsitinib
Synonyms OSI906;OSI 906;OSI-906;
Formula C26H23N5O M. Wt 421.49
  • Biological Activity
Description OSI-906 inhibits IGF-1R autophosphorylation and activation of the downstream signaling proteins Akt, ERK1/2 and S6 kinase with IC50 of 0.028 to 0.13 μM. OSI-906 enables an intermediate conformation of the target protein through interactions with the C-helix. OSI-906 displays favorable metabolic stability in liver microsomes. OSI-906 fully inhibits both IR and IGF-1R phosphorylation at a concentration of 1 μM. OSI-906 inhibits proliferation of several tumor cell lines including non-small-cell lung cancer and colorectal cancer (CRC) tumor cell line with EC50 of 0.021 to 0.810 μM.
Pathways Angiogenesis/Protein Tyrosine Kinase 
Targets Insulin Receptor IGF1R 

Structure

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