Linsitinib

- Overview
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    Background
    
    Linsitinib (OSI-906) is a potent and novel small-molecule inhibitor inhibiting insulin receptor (IR) and IGF-1 receptor (IGF-1R) kinases with IC50 value of 75nM and 35nM, respectively1.
    Studies in 3T3/hulGF-1R(LISN) cells showed that linsitinib inhibits the ligant-dependent autophosphorylation of IGF-1R and its downstream signaling pathways including pERK1/2, pAKT, p-p70S6K. Linsitinib showed anti-proliferative effects in different cancer cell lines including colorectal cells (SW620), breast tumor cells (DY4475) and mouse fibroblast cells (3T3/hulGF-1R) with EC50 of 21nM, 86nM, and 78nM, respectively1.
    Linsitinib administrated orally in LISN derived xenograft model has been shown to suppress the tumor growth in a dose-dependent manner 1.
    
    1. Mulvihill MJ1, Cooke A, Rosenfeld-Franklin M, Buck E, Foreman K, Landfair D, O'Connor M, Pirritt C, Sun Y, Yao Y, Arnold LD, Gibson NW, Ji QS. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med Chem. 2009 Sep;1(6):1153-71
- Properties
  - Alternative Name
    
    OSI 906; OSI-906; OSI906; 3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol
    
    CAS Number
    
    867160-71-2
    
    Molecular Formula
    
    C26H23N5O
    
    Molecular Weight
    
    421.51
    
    Appearance
    
    A solid
    
    Purity
    
    99.13%
    
    Solubility
    
    ≥21.08 mg/mL in DMSO; insoluble in H2O; ≥2.88 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Sean ross,Rotwein. "Methods of selecting akt agonists or antagonists." US Patent App. 15/085,757, 2016.
    2. Gross SM, Rotwein P. "Unraveling Growth Factor Signaling and Cell Cycle Progression in Individual Fibroblasts." J Biol Chem. 2016 Jul 8;291(28):14628-38. PMID:27226630
    3. Gross SM, Rotwein P. "Mapping growth-factor-modulated Akt signaling dynamics." J Cell Sci. 2016 May 15;129(10):2052-63. PMID:27044757