Marbotinib is a highly potent, specific, next-generation FLT3 inhibitor.
Marbotinib induced 91% cell death in MV4-11 cells (IC50=3 nM) at 5 nM in comparison with quizartinib (IC50 3 nM) and FLT3i-469 (IC50 4 nM).
Marbotinib is a low-nanomolar and highly specific inhibitor of mutant FLT3 and of the growth of AML cells with FLT3-ITD and FLT3-TKD mutations.
Marbotinib suppresses the phosphorylation of FLT3-ITD and the growth of permanent and primary AML cells with FLT3-ITD, Marbotinib shows high selectivity for FLT3 and alters signaling, reminiscent of genetic elimination of FLT3-ITD.
The water-soluble marbotinib-carbamate significantly prolongs survival of mice with FLT3-driven leukemia.
