Preferred Label : Segigratinib;
NCIt synonyms : FGFR/CSF-1R Inhibitor 3D185;
NCIt definition : An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) types
1, 2, and 3 (FGFR1/2/3) and colony stimulating factor 1 receptor (CSF1R; CSF-1R; CD115;
M-CSFR), with potential immunomodulatory and antineoplastic activities. Upon administration,
segigratinib binds to and inhibits FGFR1/2/3, which may result in the inhibition of
FGFR1/2/3-mediated signal transduction pathways. This inhibits proliferation in FGFR1/2/3-overexpressing
tumor cells. 3D185 also targets and binds to CSF1R, thereby blocking CSF1R activation
and CSF1R-mediated signaling. This inhibits the activities of tumor-associated macrophages
(TAMs) and myeloid-derived suppressor cells (MDSCs), and prevents immune suppression
in the tumor microenvironment (TME). This enhances antitumor T-cell immune responses
and inhibits the proliferation of tumor cells. FGFR, a family of receptor tyrosine
kinases (RTKs) upregulated in many tumor cell types, plays a key role in cellular
proliferation, migration and survival. CSF1R, also known as macrophage colony-stimulating
factor receptor (M-CSFR) and CD115 (cluster of differentiation 115), is a cell-surface
receptor that plays major roles in tumor cell proliferation and metastasis.;
UNII : G0Z5E4YTB4;
CAS number : 1882873-93-9;
Molecule name : 3D-185; HH185; 3D 185;
NCI Metathesaurus CUI : CL1412860;
Origin ID : C175460;
UMLS CUI : C5446541;
Semantic type(s)
- concept_is_in_subset
- has_target
