Preferred Label : RAS/PI3K-alpha Interaction Inhibitor BBO-10203;
NCIt synonyms : PI3K-alpha:RAS Breaker BBO-10203; RAS-driven PI3K-alpha Inhibitor BBO-10203; RAS/PI3Ka Interaction Inhibitor BBO-10203; PI3Ka:RAS Breaker BBO-10203;
NCIt definition : An orally bioavailable covalent small molecule inhibitor of RAS-driven phosphatidylinositol
4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3K-alpha; PI3Ka; PIK3CA)
activity, with potential antineoplastic activity. Upon oral administration, RAS/PI3Ka
interaction inhibitor BBO-10203 disrupts the interaction between RAS and PIK3CA, thereby
inhibiting PIK3CA in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin
(mTOR) pathway. This results in apoptosis and growth inhibition in PIK3CA-expressing
tumor cells. By specifically targeting RAS-mediated activation of the PI3K/Akt/mTOR
pathway, BBO-10203 may not cause hyperglycemia associated with direct PIK3CA kinase
inhibition. 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 : BBO-10203; BBO 10203;
Origin ID : C211917;
concept_is_in_subset
- has_target
