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Erlotinib inhibits EGFR tyrosine kinase auto-phosphorylation. Studies in cell lines and enzyme assays have shown that erlotinib inhibits EGFR at concentrations significantly lower than those needed to inhibit c-src and v-abl. It has an IC50 of 2 nM against EGFR. It is >1000-fold more sensitive for EGFR than for c-Src or v-Abl.
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