GDC-0349 是一种有效的，ATP竞争性的选择性 mTOR 抑制剂，K_i 值为 3.8 nM。GDC-0349 抑制 mTORC1 和 mTORC2 复合体。

GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a K i of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.

Solid

mTOR 3.8 nM (Ki) mTORC1

GDC-0349 (Compound 8h) is a remarkably selective mTOR inhibitor, with less than 25% inhibition of 266 kinases, including all isoforms of PI3K when tested at 1 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 (Compound 8h) inhibits tumor growth in a dose-dependent manner, achieving stasis (99% TGI) at the maximum tolerated dose. Body weight change is less than 10% up to the highest dose. GDC-0349 is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). Similar levels of tumor growth inhibition are achieved when GDC-0349 is administered once every three days at higher doses compared to once every day. GDC-0349 has ~10-fold reduced free plasma clearance in both mice (100 mL/min/kg) and rats (171 mL/min/kg in rat). has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Pei Z, et al. Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7.

In Vitro: DMSO : ≥ 100 mg/mL (220.97 mM)配制储备液