产品描述:
PF-04979064 is a dual inhibitor of PI3K and mTOR (Kis = 0.13, 0.111, 0.122, and 1.42 nM for PI3Kα, PI3Kγ, PI3Kδ, and mTOR, respectively).{51505} It is selective for PI3K and mTOR over a panel of 36 other kinases at 1 µM. PF-04979064 inhibits phosphorylation of Akt in BT-20 breast cancer cells (IC50 = 9.1 nM). It reduces tumor volume by 88% in a U87MG glioblastoma mouse xenograft model when administered at a dose of 40 mg/kg. PF-04979064 also increases alveolar epithelial cell apoptosis in a mouse model of chronic obstructive pulmonary disease (COPD) induced by fine particulate matter less than 2.5 µm (PM2.5).{51504}