"目录号: HY-15248
GDC-0349是ATP竞争性mTOR抑制剂，Ki为3.8 nM，比对PI3Kα和其它266种激酶的抑制性高超过700倍。
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生物活性
Description
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3Kα and other 266 kinases.IC50 value: 3.8 nMTarget: mTORGDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-O (VHL mutant).
Clinical Trial
Genentech, Inc.
Non-Hodgkin's Lymphoma, Solid Tumor
June 2011
Phase 1
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