产品描述:
GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase α (PI3Kα; Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively.{43203} It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.{43204}