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Cat. No. Name Size Price Add Cart
KI0433CI-1033 (Canertinib)10 mg$112
CI-1033 (Canertinib)25 mg$272
CI-1033 (Canertinib)50 mg$432
CI-1033 (Canertinib)200 mg$1072

Chemical Characteristic

Product NameCI-1033 (Canertinib)
SynonymsCanertinib
CAS No.267243-28-7
Molecular Weight 485.94
FormulaC24H25ClFN5O3
Chemical NameN-[4-(3-Chloro-4-fluoroanilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide
SmilesC(=O)(C=C)Nc1cc2c(ncnc2cc1OCCCN1CCOCC1)Nc1cc(c(cc1)F)Cl
Chemical Structure

Biological activities

CI-1033 is an irreversible Pan-erbB tyrosine kinase inhibitor. IC50 value of CI-1033 is approximately 10 nM for erbB kinases.[1] CI-1033 reveals prominent anticancer activity in a broad range of in vivo and in vitro assessments. In the human tumor cloning assay, CI-1033 prevention the growth of clonogenic cells derived from a variety of tissue types.[2] CI-1033 efficiently blocks signal transduction through all four members of the erbB receptor family. In addition, CI-1033 covalently binds to these receptors, irreversibility inhibiting them. Thereby, CI-1033 provides prolonged suppression of erbB receptor-mediated signaling.[3] CI-1033 at a concentration of 2 μM induces accumulation of Jurkat cells in the G1 cell cycle phase and increases doses induced apoptosis in a time-dependent manner.[4] Exposure of LoVo and Caco-2, but not SW620 cells, to CI-1033 in the range of 1?? μM blocks constitutive signaling by tyrosine kinases, arrests cell growth. Additionally, CI-1033 inhibits cells in G1, stimulates expression of p53, and induces apoptosis. Both 1 and 3 μM CI-1033 blocks phosphorylation for prolonged time periods. Substantial inhibition of phosphorylation of receptor tyrosine kinases is observed by 30 min after exposure to 3 μM CI-1033 and continued for up to 24 hours in the presence of CI-1033. Both 1 and 3 μM CI-1033 blocks phosphorylation for prolonged time periods. Substantial inhibition of phosphorylation of receptor tyrosine kinases is observed by 30 min after exposure to 3 μM CI-1033 and continued for up to 24 hours in the presence of CI-1033. CI-1033-induced G1 arrest is not observed in SW620 cells. CI-1033 produces a modest increase in radiosensitivity of Caco-2 and LoVo cells whereas SW620 cells are not sensitized. The combination of CI-1033 and radiation generates marked and prolonged inhibition of tumor growth in both the tumor types when compared with either treatment alone. [2]

Protocols

CI-1033 is dissolved in water and is given orally in the morning. [2]

References

[1] Kumar-Sinha C, et al. Transcriptome analysis of HER2 reveals a molecular connection to fatty acid synthesis. Cancer Res. 2003, 63(1): 132-139.
[2] Nyati MK, et al. Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo. Clin Cancer Res. 2004, 10(2): 691-700.
[3] Allen LF, et al. CI-1033, an irreversible pan-erbB receptor inhibitor and its potential application for the treatment of breast cancer. Semin Oncol. 2003, 30(5 Suppl 16): 65-78.
[4] Trinks C, et al. The pan-ErbB tyrosine kinase inhibitor canertinib induces caspase-mediated cell death in human T-cell leukemia (Jurkat) cells. Biochem Biophys Res Commun. 2011, 410(3): 422-427.

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