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Biological Activity:
EGFR inhibitor; Erlotinib inhibits EGFR tyrosine kinase autophosphorylation by inhibition of the intracellular domain. Studies in cell lines and enzyme assays have both shown that erlotinib inhibits EGFR at concentrations significantly lower than those needed to inhibit c-src and v-abl.
References: online 1, 2
J.R. Johnson et al. Approval Summary for Erlotinib for Treatment of Patients with Locally Advanced or Metastatic Non–Small Cell Lung Cancer after Failure of at Least One Prior Chemotherapy Regimen. Clin. Can. Res. 2005, 11, 6414-6421.
J. Porter et al. A dose escalation and pharmacokinetic (PK) trial of weekly docetaxel combined with daily erlotinib in adult cancer patients. J. Clin. Oncol. 2004, 22, 14S, 2119.
Chemical Name: [6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine hydrochloride
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