Preferred Label : Flonoltinib Maleate;
NCIt definition : The maleate salt form of flonoltinib, an orally bioavailable dual inhibitor of both
Janus-associated kinase 2 (JAK2) and of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1;
FLK2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
Upon oral administration, flonoltinib targets, binds to and inhibits the activity
of both JAK2 and FLT3. This prevents the activation of the JAK/signal transducer and
activator of transcription (STAT) signaling pathway and the activation of STAT3 and
STAT5 as well as FLT3-mediated signaling. This may lead to an induction of apoptosis
and a decrease in proliferation of tumor cells in which JAK2 and FLT3 are overexpressed.
In addition, as JAK2 and FLT3 play a key role in the regulation of the inflammatory
response and dendritic cell (DC) proliferation, differentiation and function, inhibition
of JAK2- and FLT3-mediated signaling may suppress the generation and differentiation
of DCs, and may regulate inflammatory and immune responses. JAK2, often upregulated
or mutated in a variety of cancer cells, mediates STAT3 activation and plays a key
role in tumor cell proliferation and survival. FLT3, a class III receptor tyrosine
kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute
myeloid leukemias.;
NCI Metathesaurus CUI : CL1778270;
Origin ID : C185862;
UMLS CUI : C5670116;
Semantic type(s)
- concept_is_in_subset
- has_target
