TL 0259 is a selective and highly potent Fgr and Lyn inhibitor (IC50 values are 0.03 and 0.1 nM, respectively). Exhibits selectivity for Fgr and Lyn over other Src family kinases and other nonreceptor and receptor tyrosine kinases. Suppresses proliferation of acute myelogenous leukemia (AML) cell lines in vitro. Eliminates leukemic cells from spleen and bone of mice bearing AML xenografts. Orally bioavailable.
