Preferred Label : Mutant-selective PI3K-alpha Inhibitor BPI-21668;
NCIt synonyms : PIK3CA Inhibitor BPI-21668; PI3K-alpha Inhibitor BPI-21668;
NCIt definition : An orally bioavailable, small molecule inhibitor of the class I phosphatidylinositol-4,5-bisphosphate
3-kinase (PI3K) catalytic subunit alpha (PIK3CA; PI3K p110alpha) mutant(s), with potential
antineoplastic activity. Upon oral administration, PI3K-alpha inhibitor BPI-21668
selectively targets, binds to and inhibits the activity of PIK3CA mutant(s), in the
PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results
in both apoptosis and growth inhibition in PIK3CA mutant-expressing tumor cells. Dysregulation
of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion
of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA,
one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit
of the class I PI3K.;
Molecule name : BPI 21668; BPI-21668;
NCI Metathesaurus CUI : CL1792158;
Origin ID : C187350;
UMLS CUI : C5706414;
Semantic type(s)
- concept_is_in_subset
- has_target
