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 vitro and in vivo in animal models of chronic myelogenous leukemia.^2,3,4

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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).