Preferred Label : Sotuletinib Dihydrochloride;
NCIt synonyms : BLZ945 Dihydrochloride; BLZ 945 Dihydrochloride; 2-Pyridinecarboxamide, 4-((2-(((1r,2r)-2-Hydroxycyclohexyl)amino)-6-Benzothiazolyl)oxy)-N-methyl-,
Hydrochloride (1:2); BLZ-945 Dihydrochloride;
NCIt definition : An orally bioavailable inhibitor of colony stimulating factor 1 receptor (CSF-1R;
CSF1R), with potential antineoplastic activity. CSF1R inhibitor BLZ945 selectively
binds to CSF1R expressed on tumor-associated macrophages (TAMs), blocks the activity
of CSF1R, and inhibits CSF1R-mediated signal transduction pathways. This inhibits
the activity and proliferation of TAMs, and reprograms the immunosuppressive nature
of existing TAMs. Altogether, this reduces TAM-mediated immune suppression in the
tumor microenvironment, re-activates the immune system, and improves anti-tumor cell
responses mediated by T-cells. CSF1R, also known as macrophage colony-stimulating
factor receptor (M-CSFR) and CD115 (cluster of differentiation 115), is a cell-surface
receptor for its ligand, colony stimulating factor 1 (CSF1); this receptor is overexpressed
by TAMs in the tumor microenvironment, and plays a major role in both immune suppression
and the induction of tumor cell proliferation.;
UNII : QJE0UTG9TS;
CAS number : 2222138-40-9;
NCI Metathesaurus CUI : CL1771396;
Origin ID : C183175;
UMLS CUI : C5667125;
Semantic type(s)
- concept_is_in_subset
