FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase ( FAK ) inhibitor with an IC 50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice.