Description
Erlotinib (CP-358,774) can inhibit EGFR with IC50 of 2 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C22H24CLN3O4
Chemical Name
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride
Solubility
DMSO 3 mg/mL Water
In vitro
As a potent EGFR inhibitor, erlotinib (CP-358,774) shows a great inhibition to EGFR. Erlotinib (CP-358,774) can inhibit EGFR with IC50 of 2 nM by bind to the adenosine triphosphate (ATP) binding site of EGFR. As triphosphate (ATP) binding site of EGFR does not work, autophosphorylation of EGFR is blocked by Erlotinib. For cell lines (1)The proliferation of DiFi cells is strongly inhibited by Erlotinib (CP-358,774) with an IC50 of 100 nM. (2)The HN5 human head and neck tumor cell line, which also expresses a very high level of the EGFR, is markedly inhibited by CP-358,774 at concentrations as low as 50 nM and is completely blocked at 250 nM. (3)Erlotinib shows great inhibition to NSCLC. (4) Erlotinib inhibits the proliferation of DiFi human colon tumor cells at submicromolar concentrations in cell culture and blocks cell cycle progression at the G1 phase.
In vivo
In vivo studies show that erlotinib has activity against human colorectal, head and neck, non-small cell lung, and pancreatic tumor cells
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