BMS-554417

• CAS Number :

  468741-42-6

• Target :

  Others

• Related Pathways :

  Others

• Bioactivity :

  BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 for proliferation ranged from 120 nmol/L (Colo205) to >8.5 micromol/L (OV202) . BMS-554417 treatment inhibited IGF-IR and insulin receptor signaling through extracellular signal-related kinase as well as the phosphoinositide 3-kinase/Akt pathway, as evidenced by decreased Akt phosphorylation at Ser473. At doses that inhibited proliferation, the compound also caused a G0-G1 arrest and prevented nuclear accumulation of cyclin D1 in response to LR3 IGF-I. In Jurkat T-cell leukemia cells, this agent triggered apoptotic cell death via the mitochondrial pathway. BMS-554417 was orally bioavailable and significantly inhibited the growth of IGF1R-Sal tumor xenografts in vivo. BMS-554417 is a member of a novel class of IGF-IR/insulin receptor inhibitors that have potential......

• Smiles :

  N(C[C@@H](O)C1=CC(Cl)=CC=C1)C2=C(C=3NC=4C(N3)=CC(=CC4C)N5CCN(CCC#N)CC5)C(=O)NC=C2

• Molecular Formula :

  C28H30ClN7O2

• Molecular Weight :

  532.04

• Shipping Conditions :

  Cool pack

• Storage Temperature :

  -20°C