Erlotinib, Hydrochloride Salt (Tarceva, CP-358774, OSI-774, RO508231, CAS 183319-69-9), >99%

LC Laboratories' Product Number E-4007 - Erlotinib, Hydrochloride Salt (Tarceva, CP-358774, OSI-774, RO508231), >99% - for research use only. Inhibitor of the epidermal growth factor receptor tyrosine kinase, which is highly expressed and occasionally mutated in various forms of cancer. Erlotinib binds reversibly to the ATP binding site of the receptor. Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylatlon in tumor cells (IC50 = 20 nM). Erlotinib has been shown to be a potent inhibitor of JAK2-V617F, a mutant of tyrosine kinase JAK2 found in a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia and most patients with polycythemia vera (PV). The study indicates that erlotinib may be used to treat JAK2-V617F-positive PV and other myeloproliferative disorders. Found to be a potent inhibitor of EGFR kinase (Ki = 0.7 nM), but much weaker for ErbB-2 kinase (Ki = 1 µM) and ErbB-4 kinase (Ki = 1.5 µM). Erlotinib is the active ingredient in the drug sold under the trade name Tarceva®. This drug has been approved in at least one country for use in patients with pancreatic cancer, non-small cell lung cancer and several other types of cancer.

• Supplier: LC Laboratories
• Product #: E-4007
• Sku #: E-4007_2g