产品描述:
T5601640 is an inhibitor of LIM kinase 2 (LIMK2) that inhibits LIMK2-mediated cofilin phosphorylation.{41239} It reduces the levels of phosphorylated cofilin (p-cofilin) in mouse embryonic fibroblasts (MEF) lacking neurofibromin (Nf1-/-; IC50 = 30 µM), which normally have high levels of p-cofilin. T5601640 (50 µM) decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation of Nf1-/- MEF cells. It inhibits proliferation of ST88-14, U87, and PANC-1 cells with IC50 values of 18.3, 7.4, and 35.2 µM, respectively, and also decreases p-cofilin levels by 20, 24, and 46%, respectively.{41240} Oral gavage administration of T5601640 (60 mg/kg) decreases tumor volume and cofilin phosphorylation in a PANC-1 nude mouse xenograft model.