产品描述:
SBI-0640756 is an inhibitor of eukaryotic translation initiation factor 4 gamma 1 (eIF4G1).{69714} It inhibits the association of eIF4G1 with the eIF4F complex in UACC-903 melanoma cell lysates in an m7GTP-agarose pull-down assay when used at a concentration of 0.75 µM. SBI-0640756 also inhibits eIF4G1-dependent and -independent mRNA translation in reporter assays using rabbit reticulocyte lysates (IC50s = 3.83 and 4.59 µM, respectively). It reduces the growth of 1205Lu, WM1346, A375, UACC-903, and WM3629 melanoma cells in a concentration-dependent manner. SBI-0640756 (0.5 mg/kg) decreases tumor incidence by 50% in an N-RasQ61K-expressing, Ink4a-/- murine melanoma model. It also decreases tumor volume in an A375 mouse xenograft model when used in combination with the B-RAFV600E inhibitor PLX4720 (Item No. 15142).