产品描述:
GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR; Ki = 3.8 nM).{41444} It is selective for mTOR over a panel of 266 kinases at a concentration of 1 μM. GDC-0349 inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in head and neck squamous cell carcinoma (HNSCC) cells via inhibition of mTOR complex 1 (mTORC1) and mTORC2 and induction of autophagy.{41444,41445} Oral administration of GDC-0349 (10-80 mg/kg) inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner. It also reduces tumor growth in an A549 lung cancer mouse xenograft model when administered in combination with the PI3K inhibitor GDC-0941 (Item No. 11600) or the MEK inhibitor cobimetinib (GDC-0973; Item No. 19563).