Orally active dual FAK/PYK2 inhibitor (IC50 value 1.5 nM and ~100 nM in vitro and in vivo, respectively) that blocks FAK and p130Cas (130 kDa Crk-associated substrate) tyrosine phosphorylation, promotes caspase-3 activation, and selectively triggered cell apoptosis in tumor cells in 3D environments. PND1186 inhibitory effects differ from Dasatinib (Axon 1392; as it does not affect c-Src activity), and prevents spontaneous breast to lung metastasis in pre-clinical models. PND-1186 inhibits cell growth in multiple myeloma (MM) cells both in vitro and in vivo by inhibition of PYK2 (IC50 and EC50 values 85 nM and 20 nM, respectively).