PD 166326

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 Res. 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. Clin. Cancer Res. 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. Proc. Natl. Acad. Sci. USA 103(24), 9244-9249 (2006).