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- NCIT_C198692 IAO_0000115 "An orally bioavailable, covalent inhibitor of class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA; PI3K p110alpha), with potential antineoplastic activity. Upon oral administration, PI3K-alpha inhibitor TOS-358 selectively targets, binds to and covalently inhibits wild-type PIK3CA and its mutated forms in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting PIK3CA, this agent may be more efficacious and less toxic than pan-PI3K inhibitors. 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_C198692 NCIT_A7 NCIT_C30168 @default.
- NCIT_C198692 NCIT_NHC0 "C198692" @default.
- NCIT_C198692 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C198692 NCIT_P107 "PI3K-alpha Inhibitor TOS-358" @default.
- NCIT_C198692 NCIT_P108 "PI3K-alpha Inhibitor TOS-358" @default.
- NCIT_C198692 NCIT_P322 "CTRP" @default.
- NCIT_C198692 NCIT_P322 "GDC" @default.
- NCIT_C198692 NCIT_P399 "812126" @default.
- NCIT_C198692 normalizedInformationContent "100" @default.
- NCIT_C198692 referenceCount "1" @default.
- NCIT_C198692 hasExactSynonym "PI3K-alpha Inhibitor TOS-358" @default.
- NCIT_C198692 hasExactSynonym "PI3Kalpha Inhibitor TOS-358" @default.
- NCIT_C198692 hasExactSynonym "TOS 358" @default.
- NCIT_C198692 hasExactSynonym "TOS-358" @default.
- NCIT_C198692 hasExactSynonym "TOS358" @default.
- NCIT_C198692 inSubset NCIT_C116977 @default.
- NCIT_C198692 inSubset NCIT_C116978 @default.
- NCIT_C198692 inSubset NCIT_C128784 @default.
- NCIT_C198692 inSubset NCIT_C157711 @default.
- NCIT_C198692 inSubset NCIT_C157712 @default.
- NCIT_C198692 inSubset NCIT_C176424 @default.
- NCIT_C198692 type Class @default.
- NCIT_C198692 isDefinedBy ncit.owl @default.
- NCIT_C198692 label "PI3K-alpha Inhibitor TOS-358" @default.
- NCIT_C198692 subClassOf NCIT_C129824 @default.
- NCIT_C198692 subClassOf NCIT_C129825 @default.
- NCIT_C198692 subClassOf NCIT_C1404 @default.
- NCIT_C198692 subClassOf NCIT_C163758 @default.
- NCIT_C198692 subClassOf NCIT_C1742 @default.
- NCIT_C198692 subClassOf NCIT_C1908 @default.
- NCIT_C198692 subClassOf NCIT_C1909 @default.
- NCIT_C198692 subClassOf NCIT_C198692 @default.
- NCIT_C198692 subClassOf NCIT_C2152 @default.
- NCIT_C198692 subClassOf NCIT_C2189 @default.
- NCIT_C198692 subClassOf NCIT_C274 @default.
- NCIT_C198692 subClassOf NCIT_C471 @default.