Preferred Label : Itacnosertib;
NCIt synonyms : ALK2 Inhibitor TP-0184; ACVR1 Inhibitor TP-0184; ALK-2 Inhibitor TP-0184;
NCIt definition : An orally bioavailable inhibitor of activin A receptor type 1 (activin receptor-like
kinase 2; ALK2; ALK-2; ACRV1), with potential antineoplastic activity. Upon oral administration,itacnosertib
targets, binds to and inhibits the activity of ALK-2. This prevents ALK-2-mediated
signaling and inhibits cell growth in ALK-2-overexpressing tumor cells. In addition,
in cancer and inflammatory conditions, ALK-2 is upregulated in response to increased
signaling of pro-inflammatory cytokines, especially interleukin-6 (IL-6), and enhances
the secretion of hepcidin, a peptide liver hormone and a key modulator of iron homeostasis.
Blocking ALK-2-mediated pathways in inflammation and cancer leads to a decrease of
hepcidin expression and restores plasma iron levels, thereby preventing low serum
iron levels and anemia of chronic disease (ACD). ALK-2, a serine/threonine receptor
kinase, is constitutively activated due to activating mutations or upregulated upstream
signaling pathways in inflammatory conditions and certain types of cancer.;
UNII : 22Z53X5LHF;
InChIKey : XSQKEVGTZSBVBR-UHFFFAOYSA-N;
CAS number : 1628870-27-8;
Molecule name : TP 0184; TP-0184;
NCI Metathesaurus CUI : CL935854;
Origin ID : C156729;
UMLS CUI : C5446333;
Semantic type(s)
- concept_is_in_subset
- has_target
