• 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, METHANESULFONATE SALT RESEARCH COMPOUND 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, medical, 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.

Related Terms:

[Gleevec] [Glivec] [Genfatinib]M.W. 589.71C29H31N7O•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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