| 货号 | 9084S |
| 供应商 | CST |
| 背景 | Imatinib is a tyrosine kinase (TK) inhibitor that is a relatively specific ATP-binding site antagonist of Bcr-Abl, PDGF receptor, and c-Kit TKs (1-3). Results are encouraging in chronic myeloid leukemia (CML) clinical trials and imatinib has become a paradigm for targeted cancer therapeutics (4-6). Signal transduction through phospho-tyrosine pathways has been studied extensively, and tyrosine phosphorylation has been linked to multiple cell growth and differentiation pathways (7-9). Because the observed leukemic state of CML is dependent on the intact Bcr-Abl tyrosine kinase activity, extensive work has been done to identify substrates of Bcr-Abl and thus possible mechanisms leading to a myeloid expansion. Many groups have characterized prominent tyrosine-phosphorylated protein substrates in both CML blasts and Bcr-Abl-expressing cell lines, including SHIP, c-Cbl, Dok, Shc, and CrkL (10-15). In addition, key signal transduction pathways involving PI3 kinase, Ras, Myc, and Stat5 are also activated in a Bcr-Abl kinase-dependent manner (16). |
| 存放说明 | -20C |
| 参考文献 | 1 . Buchdunger, E. et al. (1996) Cancer Res 56, 100-4. 2 . Heinrich, M.C. et al. (2000) Blood 96, 925-32. 3 . Blume-Jensen, P. and Hunter, T. (2001) Nature 411, 355-65. 4 . Druker, B.J. et al. (1996) Nat Med 2, 561-6. 5 . Mauro, M.J. and Druker, B.J. (2001) Curr Oncol Rep 3, 223-7. 6 . Druker, B.J. et al. (2001) N Engl J Med 344, 1031-7. 7 . Druker, B.J. et al. (2001) N Engl J Med 344, 1038-42. 8 . Ullrich, A. and Schlessinger, J. (1990) Cell 61, 203-12. 9 . Cantley, L.C. et al. (1991) Cell 64, 281-302. 10 . ten Hoeve, J. et al. (1994) Blood 84, 1731-6. 11 . Matsuguchi, T. et al. (1994) J Biol Chem 269, 5016-21. 12 . Carpino, N. et al. (1997) Cell 88, 197-204. 13 . Sattler, M. et al. (1997) Oncogene 15, 2379-84. 14 . Di Cristofano, A. et al. (1998) J Biol Chem 273, 4827-30. 15 . Wisniewski, D. et al. (1999) Blood 93, 2707-20. 16 . Kabarowski, J.H. and Witte, O.N. (2000) Stem Cells 18, 399-408. |
Chemical structure of imatinib.伊马替尼的化学结构。 | |
Western blot analysis of extracts from K-562 cells, untreated (-) or treated with imatinib (10 μM, 1 hr; +), using PathScan® Bcr/Abl Activity Assay: Phospho-c-Abl, Phospho-Stat5 and Phospho-CrkL Multiplex Western Detection Cocktail #5300 to detect inhibition of phospho-Bcr-Abl, phospho-Stat5, and phospho-CrkL.Western blot分析K-562细胞提取物，未处理(-)或用伊马替尼(10 μM, 1小时; +)处理，使用PathScan® Bcr/Abl活性分析：用磷酸-c-Abl，磷酸-Stat5和磷酸-CrkL Multiplex Western Detection Cocktail #5300来检测磷酸-Bcr-Abl，磷酸-Stat5和磷酸-CrkL的抑制。 |
