Linsitinib is an imidazopyrazine with substituents at positions 1, 3, and 8: 2-phenylquinolin-7-yl, cis-3-hydroxy-3-methylcyclobutyl, and amino groups, respectively. It is a dual inhibitor of the IGF-1 receptor and insulin receptor (IC50 = 35 and 75 nM) and was previously in clinical development for cancer and thyroid eye disease. It functions as an IGF-1 receptor antagonist, antimycobacterial agent, antineoplastic, and apoptosis inducer. It belongs to cyclobutanes, imidazopyrazines, quinolines, benzenes, aromatic amines, and tertiary alcohols.
