Malonoben is a synthetic inhibitor of protein tyrosine kinase (PTK) that displays characteristics of a potent reversible inhibitor of platelet-derived growth factor (PDGF)-induced mitogenesis via inhibition of tyrosine kinase activity of the PDGFR (PDGF receptor) and other signaling cascades. Malonoben significantly attenuated CCR7-induced Pyk2 tyrosine phosphorylation, activation of cofilin and sequentially abolished F-actin rearrangement, diminished the chemotaxis and migration ability of squamous cell carcinoma of the head and neck. Malonoben treatment resulted in the formation of fragmented mitochondria filament. Treatment of malonoben also evoked mitochondrial fragmentation in other cells including the neuroblastomas. Malonoben induces Drp1-mediated mitochondrial fission and apoptotic cell death.