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E-4007 Erlotinib, Hydrochloride Salt, >99%

[CP-358774] [OSI-774] [Tarceva]

M.W. 429.90

C22H23N3O4•HCl

[183319-69-9]

M.I. 14:  3672

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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• 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 sold by LC Laboratories is NOT Tarceva®, and is NOT for human use.

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.