Mitogen-activated protein kinases/extracellular signal-regulated kinase (MAPK/ERK) pathway, also known as MEK pathway, is reported to be associated with the cell proliferation, differentiation, migration, senescence and apoptosis[3]. SL327 inhibits MEK1 and MEK2, with IC50 values of 0.18 μM and 0.22 μM, respectively[4]. In vivo, the study showed that the combination of SL327 with sunitinib malate induced significant additive suppression of doxorubicin-resistant anaplastic thyroid carcinoma (ATC) tumor growth[4]. SL327 attenuates phosphorylated MAPK levels in a dose-dependent manner in mice. Administration of 10, 30, or 50 mg/kg SL327 significantly attenuates p42 phospho-MAPK levels (F=20.90, P<0.0001; 10 mg/kg SL327 vs. vehicle, P<0.05, and 30 and 50 mg/kg SL327 vs. vehicle, P<0.001). Injection with 30 or 50 mg/kg SL327 also significantly reduces p44 phospho-MAPK levels (F=5.627, P<0.005; 30 mg/kg vs. vehicle, P<0.05, and 50 mg/kg SL327 vs. vehicle, P<0.01)[5].
搜索
