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C-1201 Canertinib, Dihydrochloride Salt, >99%

[CI-1033] [PD 183805]

M.W. 558.86

C24H25ClFN5O3•2HCl

[289499-45-2]

M.I. 14:  1744

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 100 mg/mL; soluble in ethanol at 1 mg/mL with warming; soluble in water at 10 mg/mL with warming; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Compound is somewhat unstable in HPLC sample solution at room temperature.  Disposal:  A

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• 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).

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.