TG 100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.

PI3Kβ:215 nM, PI3Kα:165 nM, PI3Kγ:50 nM, PI3Kδ:24 nM

TG 100713 也强烈抑制EC增殖。[1]

Kinase Assays: PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Protein kinase assays are performed by using commercial screening services.

Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of test compounds (10 μM), and cell numbers are quantified by XTT assay.(Only for Reference)