Canertinib, Dihydrochloride (N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide Dihydrochloride, CI-1033, PD183805)

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.\n\nSolubility:\nSoluble in DMSO at 100mg/ml; soluble in ethanol at 1mg/ml with warming; soluble in water at 10mg/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.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

C1075-25

Size

25mg

Form

Supplied as an off-white to pale green powder.

Purity

~99% HPLC, TLC

References

1. Slichenmyer, W.J., et al. \"CI-1033, a pan-erbB tyrosine kinase inhibitor.\" Semin. Oncol. 28:80-85 (2001). 2. Citri, A., et al. \"Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy.\" EMBO J. 21:2407-2417 (2002). 3. INyati, M.K., et al. \"Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo.\" Clin Cancer Res. 10:691-700 (2004). 4. Fauci, A.S. and Challberg, M.D. \"Host-based antipoxvirus therapeutic strategies: turning the tables.\" J. Clin. Invest. 115:231-233 (2005). 5. 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).