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GDC-0349 (D50781)  
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2mg/580.00元
10mg/1880.00元
大包装/询价
产品编号 D50781
英文名称 GDC-0349
中文名称
别    名   mTOR抑制剂
克 隆 号
CAS 1207360-89-1
理论分子量 452.55 kDa
检测分子量
性    状 Lyophilized
保存条件 Store in dry, dark place for one year.
注意事项 This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications.
产品介绍 GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with IC50 ~3.8 nM. It has remarkable selectivity over 266 kinases, including all isoforms of PI3K (less than 25% inhibition when tested at 1 μM against Invitrogen kinase panel). 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 inhibited tumor growth in a dose-dependent manner. It was also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). GDC-0349 inhibited 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. Currently GDC-0349 is in Phase I clinical trials to evaluate the safety and tolerability in patients with locally advanced or metastatic solid tumors or Non-Hodgkin's lymphoma.

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