Preferred Label : AXL/FLT3/NTRK Inhibitor HH30134;
NCIt definition : An orally bioavailable inhibitor of multiple kinases, including the receptor tyrosine
kinases AXL (UFO) and FMS-like tyrosine kinase-3 (FLT3; CD135; fetal liver kinase-2;
Flk2), and the neurotrophic tyrosine receptor kinases (NTRKs), with potential antineoplastic
activity. Upon oral administration, AXL/FLT3/NTRK inhibitor HH30134 binds to and inhibits
wild-type, point mutants and fusion proteins of AXL, FLT3 and NTRK. 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, rearranged 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. TRK, a family of receptor tyrosine
kinases (RTKs) activated by neurotrophins, is encoded by NTRK family genes. The expression
of either mutated forms of, or fusion proteins involving, NTRK family members results
in uncontrolled TRK signaling, which plays an important role in tumor cell growth,
survival, invasion and treatment resistance.;
Molecule name : HH-30134; HH 30134; JND30134;
NCI Metathesaurus CUI : CL1662189;
Origin ID : C179578;
UMLS CUI : C5555785;
Semantic type(s)
- concept_is_in_subset
- has_target
