TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC 50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC 50 s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.