LFM-A13

LFM-A13 is an inhibitor of Bruton's tyrosine kinase (BTK; IC50 = 2.5 µM).{15125} It is selective for BTK over JAK1, JAK3, IRK, EGFR, and HCK (IC50s = >278 µM for all), as well as a panel of seven serine/threonine and 10 tyrosine kinases as well as one lipid kinase (IC50s = >200-500 µM), but does inhibit polo-like kinase 3 (PLK3; Ki = 7.2 µM) and Xenopus PLK1 (Plx1; IC50 = 10 µM).{15126,15124} LFM-A13 increases anti-FAS antibody-induced apoptosis in NALM-6-UM-1 acute lymphoblastic leukemia (ALL) cells.{15125} It reduces tumor growth in an MMTV/neu transgenic mouse model of breast cancer when administered at a dose of 50 mg/kg.{15124}