LFM-A13 is a highly specific inhibitor of BTK with Ki of 1.4 uM, IC50 of 17.2 uM, shows no activity against EGFR, IRK, JAK1, JAK3, or HCK.
LFM-A13 enhances the sensitivity to ceramide- or vincristine-induced apoptosis in BTK+ B-lineage leukemic cells; prolongs the median survival time of VPL-treated mice.
LFM-A13 also inhibits Plk3 with IC50 of 61 uM, prevented bipolar mitotic spindle assembly in human breast cancer cells and glioblastoma cells, delays tumor progression in MMTV/neu transgenic mouse model of HER2 positive breast cancer.
