An IGF-1R inhibitor
Insulin-like growth factor 1 receptor (IGF-1R) is a receptor tyrosine kinase whose activation leads to angiogenesis as well as cell proliferation, survival, transformation, and metastasis. IGF-1R signaling has been implicated in the development and progression of cancer. NVP-AEW541 is a selective IGF-1R kinase inhibitor. In vitro, it inhibits the autophosphorylation activity of IGF-1R (IC50 = 0.086 µM) and prevents IGF-1-mediated survival and proliferation of MCF-7 cells (IC50 = 0.16 and 1.64 µM, respectively). When tested against a panel of native tyrosine kinases, including the structurally-related insulin receptor (Ins-R), NVP-AEW541 is 27-fold more potent toward IGF-1R. Demonstrating positive oral bioavailabilty, NVP-AEW541 dose-dependently inhibits tumor growth in a mouse NWT-21 fibrosarcoma tumor model.
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