NCIt definition : An orally bioavailable inhibitor of two receptor tyrosine kinases (RTKs), FMS-like
tyrosine kinase-3 (Flt3; CD135; fetal liver kinase-2; Flk2) and tyrosine-protein kinase
Mer (MerTK; proto-oncogene c-Mer; Mer), with potential antineoplastic activity. Upon
administration, MRX-2843 targets and binds to both Flt3 and MerTK. This prevents ligand-dependent
phosphorylation and activation of Flt3 and MerTK, which inhibits the activation of
their downstream signaling pathways. This induces apoptosis and inhibits proliferation
of Flt3- and/or MerTK-overexpressing tumor cells. Flt3 and MerTK, are overexpressed
in certain tumor cell types and play key roles in tumor cell proliferation and survival.;
Semantic type(s)