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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/water 96/4, up to about10 mg/mL (slight warming may be needed); very slightly soluble in pure DMSO; very poorly soluble in water or ethanol.  Disposal:  A

View the MSDS for this product

• 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 is currently approved for use in patients with pancreatic cancer, non-small cell lung cancer and several other types of cancer.

• 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) Section 68B of the Patents Act of 1953 in New Zealand; (vi) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (vii) 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.