Canertinib, Dihydrochloride Salt (CI-1033, PD 183805, CAS 289499-45-2), >99%

LC Laboratories' Product Number C-1201 - Canertinib, Dihydrochloride Salt (CI-1033, PD 183805, CAS 289499-45-2), >99% - for research use only. 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. 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. Increases the effectiveness of radiation therapy. Prevents smallpox viral replication in vitro and inhibits smallpox viral infection in vivo. Canertinib inhibited erbB receptor phosphorylation and induced growth inhibition and apoptosis at concentrations of 1 µM or more.

• Supplier: LC Laboratories
• Product #: C-1201
• Sku #: C-1201_500mg