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Description: Erlotinib mesylate (also known as OSI-744 mesylate, trade name: Tarceva) is the mesylate salt of erlotinib which is an EGFR (epidermal growth factor receptor) inhibitor with IC50 of 2 nM in cell-free assays, and is > 1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib is a quinazoline derivative with potent antineoplastic properties and has been approved for the treatment of non-small cell lung cancer (NSCLC), pancreatic cancer and several other types of cancer. It acts by competing with adenosine triphosphate and reversibly binding to the intracellular catalytic domain of EGFR tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation.
References: Cancer Res. 1997; 57(21):4838-48; Anticancer Drugs. 2004; 15(5):503-12; Mol Cancer Ther. 2008; 7(6):1708-19.
Related CAS: 248594-19-6 (mesylate); 183319-69-9 (HCl); 183321-74-6 (free base)
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