An orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. FAK inhibitor PF-00562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival. As FAK is a signal transducer for integrins, inhibition of FAK by this agent may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation.