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I-5508 Imatinib, Methanesulfonate Salt, >99%

[Imatinib Mesylate] [Gleevec] [Glivec] [CGP-57148B] [STI-571]

M.W. 589.71

C29H31N7O•CH4SO3

[220127-57-1]

M.I. 14:  4902

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 100 mg/mL; very poorly soluble in ethanol; soluble in water at 200 mg/mL; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Imatinib inhibits bcr-abl tyrosine kinase activity, upon which some types of tumor cells depend for growth.  Imatinib acts by binding to the ATP binding site of bcr-abl and competitively inhibiting its tyrosine kinase activity.  Imatinib is selective for bcr-abl, but it also targets several other kinases (c-kit and PDGF-R).  Deininger, M. and Druker, B.J.  "Specific Targeted Therapy of Chronic Myelogenous Leukemia with Imatinib."  Pharmacol. Rev. 55:  401-423 (2003).

• Imatinib also stimulates the entry of the bcr-abl tyrosine kinase into the nucleus, where it cannot perform its anti-apoptopic functions.  Vigneri, P. and Wang, J.Y. "Induction of apoptosis in chronic myelogenous leukemia cells through nuclear entrapment of BCR-ABL tyrosine kinase."  Nat. Med. 7:  228-234 (2001).

• Imatinib inhibits EOL-1 cell viability (IC50 = 0.5 nM), phosphorylation of a fusion protein (IC50 = 30 nM), and viability of BaF3 cells expressing Rhe-PDGFRα in the absence of IL-3 (IC50 = 0.17 nM).  Griffin, J.H., et al.  "Discovery of a fusion kinase in EOL-1 cells and idiopathic hypereosinophilic syndrome."  Proc. Natl. Acad. Sci. USA 100:  7830-7835 (2003).

• Inhibition of CSF-1R by imatinib is competitive with ATP, with a Ki value of 120 nM.  Guo, J., et al. "Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors."  Mol. Cancer Ther. 5:  1007-1013 (2006).

• The IC50 values for imatinib inhibition of KBM5 and KBM7 cell growth were about 0.48 and 0.24 µM, respectively, while the IC50 values for imatinib in KBM5-STI571R1.0 and KBM7-STI571R1.0 cells were about 6.40 and 3.30 µM, respectively. (The data were from figure 2 but we found several errors in the figure. The correct data cannot be determined without further information).  The calculated resistance indexes for imatinib were 13.3 for KBM5-STI571R1.0 cells and 13.8 for KBM7-STI571R1.0 cells.  Golemovic, M., et al.  "AMN107, a Novel Aminopyrimidine Inhibitor of Bcr-Abl, Has In vitro Activity against Imatinib-Resistant Chronic Myeloid Leukemia."  Clin. Cancer Res. 11:  4941-4947 (2005).

• Imatinib is the active ingredient in the drug sold under the trade name Gleevec® in USA or Glivec in Europe and Australia.  This drug has been approved in at least one country for use in patients with gastrointestinal stromal tumors, chronic myelogenous leukemia and a number of other malignancies.  NOTE:  The imatinib sold by LC Laboratories is NOT Gleevec® or Glivec, 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.