PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC 50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα , PI3Kβ , PI3Kγ , PI3Kδ , respectively. PI3Kγ inhibitor 7 shows antitumor activity. PI3Kγ inhibitor 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.