Preferred Label : Bimiralisib;
NCIt synonyms : 2-Pyridinamine, 5-(4,6-Di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-;
NCIt definition : An orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor
of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
Bimiralisib inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to
a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth
inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway
promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.
As mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent
of PI3K, this agent may potentially be more potent than an agent that inhibits either
PI3K kinase or mTOR kinase. By inhibiting mTOR to a lesser extent than PI3K, PQR309
does not interfere with the mTOR-mediated negative feedback loop on PI3K signaling.
Blocking the negative feedback loop would potentially increase PI3K signaling and
decrease therapeutic efficacy.;
UNII : 6Z3QHB00LB;
InChIKey : ADGGYDAFIHSYFI-UHFFFAOYSA-N;
CAS number : 1225037-39-7; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1225037-39-7
alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo
G-SRS /a ;
Molecule name : PQR-309;
NCI Metathesaurus CUI : CL454230;
Origin ID : C111898;
UMLS CUI : C4682395;
Semantic type(s)
- concept_is_in_subset
- has_target
