Preferred Label : AXL/FLT3 Inhibitor TT-00973;
NCIt definition : An orally bioavailable inhibitor of the receptor tyrosine kinases AXL (UFO) and FMS-like
tyrosine kinase-3 (FLT3; CD135; fetal liver kinase-2; Flk2), with potential antineoplastic
activity. Upon oral administration, AXL/FLT3 inhibitor TT-00973 binds to and inhibits
AXL and FLT3, including the FLT3-ITD-F691L gatekeeper mutation. Inhibition of these
kinases leads to the disruption of downstream signaling pathways and the inhibition
of cell growth of tumors in which these kinases are overexpressed or mutated. 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.;
Molecule name : TT 00973; TT-00973;
NCI Metathesaurus CUI : CL1905848;
Origin ID : C198688;
UMLS CUI : C5854361;
Semantic type(s)
- concept_is_in_subset
- has_target
