货号 | 9000988-10mg |
描述 | PD 166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases that inhibits c-abl (IC50 = 8 nM) and Bcr/Abl-dependent cell growth (IC50 = 0.4 nM).1,2 In addition to targeting a select group of receptor tyrosine kinases, PD 166326 also potently inhibits c-src (IC50 = 6 nM).2 Orally administered PD 166326 is well tolerated and effectively blocks Bcr/Abl kinase activity in vivo.3 Moreover, PD 166326 affects a distinct set of kinases from those targeted by imatinib mesylate (STI571) and can reduce the growth of some imatinib-resistant cells both in vitroandin vivo in animal models of chronic myelogenous leukemia.2,3,4 |
供应商 | Cayman |
应用文献 | |
1.Wisniewski, D.,Lambek, C.L.,Liu, C., et al. Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases. Cancer Research 62(15), 4244-4255 (2002). 2.Huron, D.R.,Gorre, M.E.,Kraker, A.J., et al. A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants. Clinical Cancer Research 9(4), 1267-1273 (2003). 3.Wolff, N.C.,Veach, D.R.,Tong, W.P., et al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood 105(10), 3995-4003 (2005). 4.Azam, M.,Nardi, V.,Shakespeare, W.C., et al. Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proceedings of the National Academy of Sciences of the United States of America 103(24), 9244-9249 (2006). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 427.3 |
分子式 | C21H16Cl2N4O2 |
CAS号 | 185039-91-2 |
稳定性 | ≥ 1 year |
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