TL02-59

TL02-59 is a small molecule phenoxyquinazoline analog that acts as a dual inhibitor of the Fms-like tyrosine kinase 3 (FLT3) and the Tyrosine-protein kinase Fes/Fps (c-Fes). Developed through research at the University of Pittsburgh and Dana-Farber Cancer Institute, it was designed to target Acute Myeloid Leukemia (AML), particularly cases involving activating mutations in FLT3. By inhibiting both FLT3 and c-Fes, TL02-59 aims to overcome the limitations of selective FLT3 inhibitors, as c-Fes has been linked to FLT3 signaling and survival in AML cells. In preclinical studies, TL02-59 demonstrated potent growth-suppressive activity and induction of apoptosis in MV4-11 AML cells, showing superior efficacy compared to inhibitors selective for c-Fes alone.