E260 (Fer and FerT inhibitor) is a Fer/FerT kinase inhibitor

Fer and FerT inhibitor, which selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. When applied to metastatic grade IV SW620 CC cells, which are serum starved for 16 h and treated with 3 mM H2O2 to activate Fer,Fer and FerT inhibitor exhibits inhibitory effects on the Fer-kinase activity as is reflected by suppressed auto-phosphorylation activity of the enzyme.

Fer/FerT kinase inhibitor suppresses xenografts progression in vivo. The pharmacokinetic (PK) profile of Fer/FerT kinase inhibitor is determined in mice. Fer/FerT kinase inhibitor exhibits a T1/2of 175 min in the blood, and a volume of distribution of 4244 mL/kg suggesting an efficient distribution of the compound in the animal tissues. To evaluate the efficacy of Fer/FerT kinase inhibitor on tumor growth, SW620 cells are subcutaneously introduced into immuno-compromised "Nude" mice. Administration of Fer/FerT kinase inhibitor leads to a significant attenuation of tumor progression throughout the experiment, and to a 10-fold decrease in average tumor volume after 22 days of treatment. To further demonstrate the anti-cancer activity of Fer/FerT kinase inhibitor in vivo, mice bearing SW48 cells derived xenografts are treated with Fer/FerT kinase inhibitor and the tumor progression profiles are determined. Mice treated with Fer/FerT kinase inhibitor demonstrate a 5-6-fold attenuation in tumors progression when compared to the control treated group