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- NCIT_C199577 IAO_0000115 "An orally bioavailable, pan-mutant selective inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (phosphoinositide 3-kinase alpha; PIK3CA; PI3K p110alpha), with potential antineoplastic activity. Upon oral administration, pan-mutant-selective PI3K-alpha inhibitor RLY-5836 selectively targets and allosterically binds to PIK3CA mutated forms, thereby preventing the activity of PIK3CA mutants. This prevents mutant PIK3CA-mediated activation of 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. By specifically targeting PIK3CA mutants, RLY-5836 may be more efficacious and less toxic than PI3K-alpha inhibitors that also inhibit the wild-type (WT) form. 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." @default.
- NCIT_C199577 NCIT_A7 NCIT_C17270 @default.
- NCIT_C199577 NCIT_NHC0 "C199577" @default.
- NCIT_C199577 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C199577 NCIT_P107 "Pan-mutant-selective PI3K-alpha Inhibitor RLY-5836" @default.
- NCIT_C199577 NCIT_P108 "Pan-mutant-selective PI3K-alpha Inhibitor RLY-5836" @default.
- NCIT_C199577 NCIT_P322 "CTRP" @default.
- NCIT_C199577 NCIT_P322 "GDC" @default.
- NCIT_C199577 NCIT_P399 "812550" @default.
- NCIT_C199577 normalizedInformationContent "100" @default.
- NCIT_C199577 referenceCount "1" @default.
- NCIT_C199577 hasExactSynonym "Mutant-selective PI3Ka Inhibitor RLY-5836" @default.
- NCIT_C199577 hasExactSynonym "PI3K-alpha Inhibitor RLY-5836" @default.
- NCIT_C199577 hasExactSynonym "PI3Ka Inhibitor RLY-2608" @default.
- NCIT_C199577 hasExactSynonym "Pan Mutant-PI3Ka Inhibitor RLY-5836" @default.
- NCIT_C199577 hasExactSynonym "Pan-mutant PI3Ka Inhibitor RLY-5836" @default.
- NCIT_C199577 hasExactSynonym "Pan-mutant-selective PI3K-alpha Inhibitor RLY-5836" @default.
- NCIT_C199577 hasExactSynonym "RLY 5836" @default.
- NCIT_C199577 hasExactSynonym "RLY-5836" @default.
- NCIT_C199577 hasExactSynonym "RLY5836" @default.
- NCIT_C199577 inSubset NCIT_C116977 @default.
- NCIT_C199577 inSubset NCIT_C116978 @default.
- NCIT_C199577 inSubset NCIT_C128784 @default.
- NCIT_C199577 inSubset NCIT_C157711 @default.
- NCIT_C199577 inSubset NCIT_C157712 @default.
- NCIT_C199577 inSubset NCIT_C176424 @default.
- NCIT_C199577 type Class @default.
- NCIT_C199577 isDefinedBy ncit.owl @default.
- NCIT_C199577 label "Pan-mutant-selective PI3K-alpha Inhibitor RLY-5836" @default.
- NCIT_C199577 subClassOf NCIT_C129824 @default.
- NCIT_C199577 subClassOf NCIT_C129825 @default.
- NCIT_C199577 subClassOf NCIT_C1404 @default.
- NCIT_C199577 subClassOf NCIT_C163758 @default.
- NCIT_C199577 subClassOf NCIT_C1742 @default.
- NCIT_C199577 subClassOf NCIT_C1908 @default.
- NCIT_C199577 subClassOf NCIT_C1909 @default.
- NCIT_C199577 subClassOf NCIT_C199577 @default.
- NCIT_C199577 subClassOf NCIT_C2152 @default.
- NCIT_C199577 subClassOf NCIT_C2189 @default.
- NCIT_C199577 subClassOf NCIT_C274 @default.
- NCIT_C199577 subClassOf NCIT_C471 @default.