• Canertinib (CI-1033, PD 183805) is a pan-erbB tyrosine kinase inhibitor. It selectively inhibits erbB1 (epidermal growth factor receptor), erbB2, erbB3, and erbB4 without blocking tyrosine kinase activity of many other receptors such as platelet-derived growth factor receptor, fibroblast growth factor receptor, and insulin receptor. Slichenmyer, W.J., et al. \"CI-1033, a pan-erbB tyrosine kinase inhibitor.\" Semin. Oncol. 28: 80-85 (2001).
• Canertinib is an irreversible tyrosine kinase inhibitor. It not only inhibits tyrosine phosphorylation but also enhances ubiquitinylation and accelerates endocytosis and subsequent intracellular destruction of ErbB-2 molecules. Canertinib alkylates a cysteine residue specific to ErbB receptors. The degradative pathway of ErbB receptor tyrosine kinases stimulated by tyrosine kinase inhibitors appears to be chaperone mediated, and thus is similar to the pathways activated by the heat shock protein 90 (Hsp90) antagonist geldanamycin and by stress-induced mechanisms. Citri, A., et al. \"Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy.\" EMBO J. 21: 2407-2417 (2002).
• Increases the effectiveness of radiation therapy. Nyati, M.K., et al. \"Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo.\" Clin Cancer Res. 10: 691-700 (2004).
• Prevents smallpox viral replication in vitro and inhibits smallpox viral infection in vivo. Fauci, A.S. and Challberg, M.D. \"Host-based antipoxvirus therapeutic strategies: turning the tables.\" J. Clin. Invest. 115: 231-233 (2005).
• Canertinib inhibited erbB receptor phosphorylation and induced growth inhibition and apoptosis at concentrations of 1 µM or more. Hughes, D.P., et al. \"Essential erbB family phosphorylation in osteosarcoma as a target for CI-1033 inhibition.\" Pediatr. Blood Cancer. 46: 614-623 (2006)
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Compound is somewhat unstable in HPLC sample solution.Disposal