Preferred Label : Denfivontinib;
NCIt definition : An orally bioavailable inhibitor of both wild type and mutant forms of FMS-like tyrosine
kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon administration,
denfivontinib binds to and inhibits the activity of FLT3, including FLT3-ITD (internal
tandem duplications), FLT3-D835Y as well as other mutants. This inhibits uncontrolled
FLT3 signaling and results in the inhibition of proliferation in tumor cells overexpressing
FLT3. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated
in most B lineage neoplasms and in acute myeloid leukemias, and plays a key role in
tumor cell proliferation. In addition, denfivontinib also inhibits, to a lesser degree,
the receptor tyrosine kinases AXL (UFO), Mer, Ret, vascular endothelial growth factor
receptor 1 (VEGFR1), Fms, fibroblast growth factor receptors (FGFR) 1 and 3, and the
serine/threonine kinases Aurora B and C.;
UNII : B06W426B66;
CAS number : 1457983-28-6;
Molecule name : G-749; G-801;
NCI Metathesaurus CUI : CL1798932;
Origin ID : C190375;
UMLS CUI : C5761760;
Semantic type(s)
- concept_is_in_subset
- has_target
