Preferred Label : Dezapelisib;
NCIt synonyms : 5H-Thiazolo(3,2-a)pyrimidin-5-one, 6-(3-Fluorophenyl)-3-methyl-7-((1S)-1-(9H-purin-6-ylamino)ethyl)-;
NCIt definition : An orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic
subunit of class I phosphoinositide-3 kinases (PI3K) with potential antineoplastic
activity. Dezapelisib specifically inhibits PI3Kdelta, which prevents both the production
of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and the activation
of the PI3K/AKT kinase signaling pathway. This decreases proliferation and induces
cell death in PI3K-overexpressing tumor cells. Unlike other isoforms of PI3K, PI3Kdelta
is often overexpressed in tumor cells, especially those of hematologic origin, and
plays a crucial role in tumor cell regulation and survival. The targeted inhibition
of PI3Kdelta allows for PI3K signaling in normal, non-neoplastic cells.;
UNII : 2K59L7G59M;
CAS number : 1262440-25-4;
Molecule name : INCB040093;
NCI Metathesaurus CUI : CL451874;
Origin ID : C107686;
UMLS CUI : C4682394;
Semantic type(s)
concept_is_in_subset
has_target