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Discovery of GDC-0068(Ipatasertib),A Selective ATP-competitive AKT Inhibitor for the Treatment of Human Tumors

James F.BlakeRui XuJosef R.BencsikDengming XiaoNicholas C.KalianStephen SchlachterIan S.MitchellKeith L.SpencerAnna L.BankaEli M.WallaceSusan L.GloorMatthew MartinsonRichard D.WoessnerGuy P.A.VigersBarbara J.BrandhuberJun LiangBrian S.SafinaJun LiBirong ZhangChristine ChabotSteven DoLeslie LeeJason OehDeepak SampathBrian B.LeeKui LinBianca M.LiedererLori FriedmanNicholas J.SkeltonBing-Yan Zhu

Genentech,USA.

摘要:Discovery of Ipatasertib(GDC-0068),an oral AKT inhibitor in Phase II clinical development,will be described.GDC-0068 is a potent,highly selective,orally bioavailable,ATP-competitive pan-AKT inhibitor,targeting AKTl,AKT2 and AKT3 with IC50 of 5 nM,18 nM and 8 nM,respectively.It demonstrates high selectivity over more than 200 screened kinases,with >100 fold selectivity for AKT over PKA.In vivo,GDC-0086 exhibited a robust anti-tumor response in xenograft models in which the PI3 K-AKT-mTOR pathway is activated.
会议名称:

BIT’s 15th Annual Congress of International Drug Discovery Science and Technology-Japan 2017(IDDST-Japan 2017)

会议时间:

2017-07-25

会议地点:

日本大阪

  • 专辑:

    医药卫生科技

  • 专题:

    药学

  • 分类号:

    R979.1

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