货号 | 12098-25mg |
描述 | Tandutinib is a potent antagonist of platelet-derived growth factor receptor β (PDGFRβ), FLT3, and c-Kit (IC50 = 200, 220, and 170 nM, respectively).1 It less potently inhibits macrophage colony-stimulating factor 1 receptor (IC50 = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.1,2 Tandutinib blocks the growth of cells expressing an internal tandem duplication within the juxtamembrane domain of the FLT3 receptor, found in some acute myelogenous leukemia cells.1,3 It also impairs the growth of colon cancer cells through its actions on the c-Kit receptor.4 Tandutinib reverses multidrug resistance in vitro by impairing the efflux activity of the multidrug resistance protein 7.5 |
别名 | CT 53518;MLN518; |
供应商 | Cayman |
应用文献 | |
1.Kelly, L.M.,Yu, J.C.,Boulton, C.L., et al. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell. 1(5), 421-432 (2002). 2.Pandey, A.,Volkots, D.L.,Seroogy, J.M., et al. Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. Journal of Medicinal Chemistry 45(17), 3772-3793 (2002). 3.Griswold, I.J.,Shen, L.J.,La Rosée, P., et al. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood 104(9), 2912-2918 (2004). 4.Ponnurangam, S.,Standing, D.,Rangarajan, P., et al. Tandutinib inhibits the Akt/mTOR signaling pathway to inhibit colon cancer growth. Molecular Cancer Therapeutics 12(5), 598-609 (2013). 5.Deng, W.,Dai, C.L.,Chen, J.J., et al. Tandutinib (MLN518) reverses multidrug resistance by inhibiting the efflux activity of the multidrug resistance protein 7 (ABCC10). Oncology Reports 29(6), 2479-2485 (2013). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 562.7 |
分子式 | C31H42N6O4 |
CAS号 | 387867-13-2 |
稳定性 | ≥ 2 years |
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