1332075-56-5Relevant academic research and scientific papers
Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf
Sutherlin, Daniel P.,Baker, Stewart,Bisconte, Angelina,Blaney, Paul M.,Brown, Anthony,Chan, Bryan K.,Chantry, David,Castanedo, Georgette,Depledge, Paul,Goldsmith, Paul,Goldstein, David M.,Hancox, Timothy,Kaur, Jasmit,Knowles, David,Kondru, Rama,Lesnick, John,Lucas, Matthew C.,Lewis, Cristina,Murray, Jeremy,Nadin, Alan J.,Nonomiya, Jim,Pang, Jodie,Pegg, Neil,Price, Steve,Reif, Karin,Safina, Brian S.,Salphati, Laurent,Staben, Steven,Seward, Eileen M.,Shuttleworth, Stephen,Sohal, Sukhjit,Sweeney, Zachary K.,Ultsch, Mark,Waszkowycz, Bohdan,Wei, Binqing
scheme or table, p. 4296 - 4302 (2012/08/13)
A potent inhibitor of PI3Kδ that is ≥200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for selectivity is illustrated through structure activity relationships and crystal structures of compounds bound to a K802T mutant of PI3Kγ. Pharmacokinetic data in rats and mice support the use of 3 as a useful tool compound to use for in vivo studies.
PYRIDO[3,2-d]PYRIMIDINE PI3K DELTA INHIBITOR COMPOUNDS AND METHODS OF USE
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Page/Page column 59, (2011/09/16)
Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
