Preferred Label : Ilginatinib;
NCIt synonyms : (S)-N-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N'-(pyrazin-2-yl)pyridine-2,6-diamine; 2,6-Pyridinediamine, N2-((1S)-1-(4-fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-2-pyrazinyl-;
NCIt definition : An orally bioavailable, small molecule inhibitor of Janus-associated kinase 2 (JAK2)
and Src-family kinases, with potential antineoplastic activity. Ilginatinib competes
with ATP for binding to JAK2 as well as the mutated form JAK2V617F, thereby inhibiting
the activation of JAK2 and downstream molecules in the JAK2/STAT3 (signal transducer
and activator of transcription 3) signaling pathway that plays an important role in
normal development, particularly hematopoiesis. In addition, ilginatinib inhibits
the Src family tyrosine kinases. This eventually leads to the induction of tumor cell
apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative
disorders (MPDs); JAK2V617F is a constitutively activated kinase that activates the
JAK/STAT signaling pathway and dysregulates cell growth and function, and its expression
transforms hematopoietic cells to cytokine-independent growth.;
UNII : 56R994WX4L;
InChIKey : UQTPDWDAYHAZNT-AWEZNQCLSA-N;
CAS number : 1239358-86-1;
Molecule name : NS-018;
NCI Metathesaurus CUI : CL430628;
Origin ID : C98109;
UMLS CUI : C5239402;
Semantic type(s)
- concept_is_in_subset
- has_target
