2. Academic Validation
  3. In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase

In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase

  • Cancer Cell. 2004 Mar;5(3):231-9. doi: 10.1016/s1535-6108(04)00051-0.
Carlos García-Echeverría 1,  Mark A Pearson,  Andreas Marti,  Thomas Meyer,  Juergen Mestan,  Johann Zimmermann,  Jiaping Gao,  Josef Brueggen,  Hans-Georg Capraro,  Robert Cozens,  Dean B Evans,  Doriano Fabbro,  Pascal Furet,  Diana Graus Porta,  Janis Liebetanz,  Georg Martiny-Baron,  Stephan Ruetz,  Francesco Hofmann
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland.
PMID: 15050915 DOI: 10.1016/s1535-6108(04)00051-0
Abstract

IGF-IR-mediated signaling promotes survival, anchorage-independent growth, and oncogenic transformation, as well as tumor growth and metastasis formation in vivo. NVP-AEW541 is a pyrrolo[2,3-d]pyrimidine derivative small molecular weight kinase inhibitor of the IGF-IR, capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. As expected for a specific IGF-IR kinase inhibitor, NVP-AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. In vivo, this orally bioavailable compound inhibits IGF-IR signaling in tumor xenografts and significantly reduces the growth of IGF-IR-driven fibrosarcomas. Thus, NVP-AEW541 represents a class of selective, small molecule IGF-IR kinase inhibitors with proven in vivo antitumor activity and potential therapeutic application.

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