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United States (Change Country)CI-1033 (Canertinib) Chemical Structure
CI-1033 (Canertinib) is an orally bioavailable irreversible Pan-erbB tyrosine kinase inhibitor, targeting EGFR with IC50 of 0.8, 19 and 7 nM for EGFR, HER-2 and ErbB-4, respectively. It effectively inhibits the growth of esophageal squamous cell carcinoma which co-expresses both EGFR and HER2 with the inhibition of phosphorylation of both MAPK and AKT. inhibitor, is a clinically promising agent that is active against all four members of the erbB receptor tyrosine kinase family. In vitro studies of human cancer cell lines indicate that CI-1033 results in prompt, potent, and sustained inhibition of tyrosine kinase activity. This inhibition is highly selective for erbB1 (epidermal growth factor receptor), erbB2, erbB3, and erbB4 without inhibiting tyrosine kinase activity of receptors such as platelet-derived growth factor receptor, fibroblast growth factor receptor, and insulin receptor, even at high concentrations. [1][2]
[1] Clin Cancer Res 2004 Nov 1;10(21):7112-20
[2] Semin Oncol 2001 Oct;28(5 Suppl 16):80-5
| Molecular Weight (WM): | 485.94 |
|---|---|
| Formula: | C24H25ClFN5O3 |
| Solubility(R.T.:25°C): | DMSO 2mg/mL |
| Water <1mg/mL | |
| Ethanol 9mg/mL |
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;Cell Cycle 8, 13, 2050-2056 CI-1033 (Canertinib) purchased from Selleck
;Cell Cycle 8, 13, 2050-2056 CI-1033 (Canertinib) purchased from Selleck
;Dr. Kian Kani of Cedars-Sinai Medical Center CI-1033 (Canertinib) purchased from Selleck
;Dr. Zhang of Tianjin Medical University CI-1033 (Canertinib) purchased from Selleck
Data from [Carcinogenes 2010;31, 1948–1955 ] CI-1033 (Canertinib) purchased from Selleck
Data from [Carcinogenesis 2010;31, 1948–1955] CI-1033 (Canertinib) purchased from Selleck
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