甲磺酸伊马替尼

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本试剂(甲磺酸伊马替尼)
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简介：
货 号：LC2-I-5508
名 称：甲磺酸伊马替尼
别 名：Imatinib Methanesulfonate Salt
C A S ：220127-57-1
分子量：589.71
分子式：C29H31N7O•CH4SO3
纯 度：HPLC/TLC:>99%
说 明：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.
文 献：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).