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Literature summary for 2.7.1.153 extracted from

  • Raynaud, F.I.; Eccles, S.; Clarke, P.A.; Hayes, A.; Nutley, B.; Alix, S.; Henley, A.; Di-Stefano, F.; Ahmad, Z.; Guillard, S.; Bjerke, L.M.; Kelland, L.; Valenti, M.; Patterson, L.; Gowan, S.; de Haven Brandon, A.; Hayakawa, M.; Kaizawa, H.; Koizumi, T.; Ohishi, T.; Patel, S.; Saghir, N.; Parker, P.; Waterfield, M.; Workman, P.
    Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases (2007), Cancer Res., 67, 5840-5850.
    View publication on PubMed
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Application

Application Comment Organism
medicine inhibitor 4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol, i.e. PI103 is inhibitory to phosphatidylinositol 3-kinases, TORC1 and DNA protein kinase. PI103 potently inhibits proliferation and invasion of a wide variety of human cancer cells in vitro and shows biomarker modulation consistent with inhibition of phosphatidylinositide 3-kinase signaling. PI103 is extensively metabolized, but distributed rapidly to tissues and tumors. This results in tumor growth delay in eight different human cancer xenograft models with various phosphatidylinositide 3-kinase pathway abnormalities. Decreased phosphorylation of AKT is observed in U87MG gliomas, consistent with drug levels achieved Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
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 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol i.e. PI103. Inhibitory to phosphatidylinositol 3-kinases, TORC1 and DNA protein kinase. PI103 potently inhibits proliferation and invasion of a wide variety of human cancer cells in vitro and shows biomarker modulation consistent with inhibition of phosphatidylinositide 3-kinase signaling Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
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 IC50 value of inhibitor 4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol is 2 nmol/l against recombinant isoform p110alpha, 3 nmol/l against recombinant isoform p110beta, 3 nmol/l against recombinant isoform p110delta, 15 nmol/l against recombinant isoform p110agamma Homo sapiens additional information