Description
CI-1033 (Canertinib) can inhibit EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C24H25ClFN5O3
Chemical Name
N-(4-(3-chloro-4-fluorophenylamino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide
Solubility
DMSO 2 mg/mL Water
In vitro
CI-1033 is an irreversible pan ErbB tyrosine kinase inhibitor, and CI-1033 inhibit all four members of the erbB receptor tyrosine kinase family by binding to the ATP-binding site in the cytoplasmic domain of the EGFR preventing autophosphorylation. CI-1033 inhibits cell proliferation in a dose-dependent manner without induction of apoptosis in human cancer cell lines. CI-1033 signi?cantly suppresses the constitutively activated AKT and the MAP kinases in MDA-MB-453 breast tumor cells.
In vivo
CI-1033 had a growth-inhibitory effect in breast cancer cells, and exposure of SUM-190PT cells to gamma ray irradiation following growth inhibition by CI-1033 enhanced the ef?cacy of ionizing radiation.
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