Preferred Label : Tenalisib;
NCIt synonyms : 4H-1-Benzopyran-4-one, 3-(3-fluorophenyl)-2-((1S)-1-(9H-purin-6-ylamino)propyl)-; 3-(3-Fluorophenyl)-2-((1S)-1-((7H-purin-6-yl)amino)propyl)-4H-1-benzopyran-4-one;
NCIt definition : An orally active, highly selective, small molecule inhibitor of the delta and gamma
isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic
activities. Upon administration, tenalisib inhibits the PI3K delta and gamma isoforms
and prevents the activation of the PI3K/AKT-mediated signaling pathway. This may lead
to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells.
In addition, this agent modulates inflammatory responses through various mechanisms,
including the inhibition of both the release of reactive oxygen species (ROS) from
neutrophils and tumor necrosis factor (TNF)-alpha activity. Unlike other isoforms
of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies
and in inflammatory and autoimmune diseases. By selectively targeting these isoforms,
PI3K signaling in normal, non-neoplastic cells is minimally impacted or not affected
at all, which minimizes the side effect profile for this agent.;
UNII : 2261HH611H;
InChIKey : HDXDQPRPFRKGKZ-INIZCTEOSA-N;
CAS number : 1639417-53-0;
Molecule name : RP-6530; RP 6530;
NCI Metathesaurus CUI : CL458227;
Origin ID : C113433;
UMLS CUI : C4743548;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
