Preferred Label : AXL/FLT3/VEGFR2 Inhibitor KC1036;
NCIt definition : An orally bioavailable inhibitor of three receptor tyrosine kinases: AXL (UFO), FMS-like
tyrosine kinase-3 (Flt3; CD135; fetal liver kinase-2; Flk2), and the vascular endothelial
growth factor receptor type 2 (VEGFR2), with potential anti-angiogenesis and antineoplastic
activities. Upon oral administration, KC1036 targets, binds to and prevents the activation
of AXL, FLT3 and VEGFR2. This blocks AXL, FLT3 and VEGFR2-mediated signal transduction
pathways, and inhibits both AXL-, FLT3- and VEGFR2-mediated proliferation of tumor
cells and the VEGFR2-mediated proliferation, survival and migration of endothelial
cells. AXL, a member of the Tyro3, AXL and Mer (TAM) family of receptor tyrosine kinases,
is overexpressed by many tumor cell types and also expressed in a variety of immune
cells including macrophages, natural killer (NK) cells, and regulatory T-cells (Tregs).
It plays a key role in tumor cell proliferation, survival, invasion and metastasis,
and is a mediator of immunosuppression. Its expression is associated with drug resistance
and poor prognosis. FLT3, a class III tyrosine kinase receptor, is overexpressed or
mutated in most B lineage and acute myeloid leukemias. VEGFR2 is frequently overexpressed
by a variety of tumor types and tumor-associated endothelial cells.;
Molecule name : KC-1036; KC 1036;
NCI Metathesaurus CUI : CL1407847;
Origin ID : C173961;
UMLS CUI : C5418039;
Semantic type(s)
- concept_is_in_subset
- has_target
