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- NCIT_C199491 IAO_0000115 "An orally bioavailable, brain penetrative, selective inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (phosphoinositide 3-kinase alpha; PIK3CA; PI3K p110alpha) mutant H1047X, with potential antineoplastic activity. Upon oral administration, mutant-selective PI3K-alpha H1047X inhibitor STX-478 selectively targets and allosterically binds to the PIK3CA mutated form PIK3CA H1047X, thereby preventing the activity of the H1047X mutant. This prevents PIK3CA H1047X-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 H1047X mutant-expressing tumor cells. By specifically targeting the PIK3CA H1047X mutation, STX-478 may be more efficacious and less toxic than other PI3K-alpha inhibitors that are not mutant specific. 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. STX-478 is able to penetrate the blood-brain-barrier (BBB)." @default.
- NCIT_C199491 NCIT_A7 NCIT_C107482 @default.
- NCIT_C199491 NCIT_NHC0 "C199491" @default.
- NCIT_C199491 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C199491 NCIT_P107 "Mutant-selective PI3K-alpha H1047X Inhibitor STX-478" @default.
- NCIT_C199491 NCIT_P108 "Mutant-selective PI3K-alpha H1047X Inhibitor STX-478" @default.
- NCIT_C199491 NCIT_P322 "CTRP" @default.
- NCIT_C199491 NCIT_P322 "GDC" @default.
- NCIT_C199491 NCIT_P399 "812753" @default.
- NCIT_C199491 normalizedInformationContent "100" @default.
- NCIT_C199491 referenceCount "1" @default.
- NCIT_C199491 hasExactSynonym "Mutant-selective PI3K-alpha H1047X Inhibitor STX-478" @default.
- NCIT_C199491 hasExactSynonym "Mutant-selective PI3Kalpha H1047X Inhibitor STX-478" @default.
- NCIT_C199491 hasExactSynonym "PIK3CA H1047X Mutant Inhibitor STX-478" @default.
- NCIT_C199491 hasExactSynonym "PIK3CA H1047X Mutation Inhibitor STX-478" @default.
- NCIT_C199491 hasExactSynonym "STX 478" @default.
- NCIT_C199491 hasExactSynonym "STX-478" @default.
- NCIT_C199491 hasExactSynonym "STX478" @default.
- NCIT_C199491 inSubset NCIT_C116977 @default.
- NCIT_C199491 inSubset NCIT_C116978 @default.
- NCIT_C199491 inSubset NCIT_C128784 @default.
- NCIT_C199491 inSubset NCIT_C157711 @default.
- NCIT_C199491 inSubset NCIT_C157712 @default.
- NCIT_C199491 inSubset NCIT_C176424 @default.
- NCIT_C199491 type Class @default.
- NCIT_C199491 isDefinedBy ncit.owl @default.
- NCIT_C199491 label "Mutant-selective PI3K-alpha H1047X Inhibitor STX-478" @default.
- NCIT_C199491 subClassOf NCIT_C129824 @default.
- NCIT_C199491 subClassOf NCIT_C129825 @default.
- NCIT_C199491 subClassOf NCIT_C1404 @default.
- NCIT_C199491 subClassOf NCIT_C163758 @default.
- NCIT_C199491 subClassOf NCIT_C1742 @default.
- NCIT_C199491 subClassOf NCIT_C1908 @default.
- NCIT_C199491 subClassOf NCIT_C1909 @default.
- NCIT_C199491 subClassOf NCIT_C199491 @default.
- NCIT_C199491 subClassOf NCIT_C2152 @default.
- NCIT_C199491 subClassOf NCIT_C2189 @default.
- NCIT_C199491 subClassOf NCIT_C274 @default.
- NCIT_C199491 subClassOf NCIT_C471 @default.