Erlotinib, Hydrochloride Salt **

产品名称：Erlotinib, Hydrochloride Salt
产品货号：LC  E-4007 
产品规格：10 G
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.  Raymond, E., et al.  "Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy."  Drugs 60 Suppl 1:  15-23, discussion 41-42 (2000).
Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM).  Moyer, J.D., et al.  "Induction of Apoptosis and Cell Cycle Arrest by erlotinib, an Inhibitor of Epidermal Growth Factor Receptor Tyrosine Kinase."  Cancer Res. 57:  4838-4848 (1997).
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.  Li, Z., et al. "Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth."  J. Biol. Chem. 282:  3428-3432 (2007).
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).  Wood, E.R., et al.  "A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib), Relationships among Protein Conformation, Inhibitor Off-Rate, and Receptor Activity in Tumor Cells."  Cancer Res. 64:  6652-6659 (2004).
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.  NOTE:  THE ERLOTINIB, HYDROCHLORIDE SALT RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT TARCEVA®, AND IS NOT FOR HUMAN USE.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 18 mg/mL with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 5-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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