ETC-206-DataSheet-MedChemExpress.pdf
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1、ETC-206Cat. No.: HY-112424CAS No.: 1464151-33-4Molecular Formula: CHNOMolecular Weight: 408.45Target: MNKPathway: MAPK/ERK PathwayStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent MNK2, IC50: 86 nMIn Vitro ETC-206 inhibits eIF4E phosphorylation in HeLa cell line with
2、an IC50 of 321 nM. The anti-proliferative effects of ETC-206 are assessed in vitro, using CellTiter-Glo viability assay against 25 hematological cancer cell lines including the K562 cell line that overexpresses eIF4E (K562 o/e eIF4E). The IC50s are 1.71 M, 3.36 M, 3.70 M, 4.81 M, 5.13 M, 5.05 M, 6.7
3、0 M, 9.76 M, and 48.8 M for SU-DHL-6, GK-5, MC 116, P3HR-1, DOHH2, MPC-11, Ramos.2G6.4C10, AHH-1, and K562 o/e eIF4E cells, respectively1.The antitumor effect of ETC-206 is then assessed in a K562 e/o eIF4E mouse xenograft model after oral administration at 25, 50, or 100 mg/kg alone or in combinati
4、on with a 2.5 mg/kg fixed dose of Dasatinib throughout the study. Dasatinib at 2.5 mg/kg elicits a tumor growth inhibition (TGI) of 88% with one tumor-free animal. In In VivoProduct Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1contrast, ETC-206 alone only yields a maximum TGI of 23%
5、at the highest administered dose of 100 mg/kg, which does not impede tumor growth, and is similar to the nontreated animals. ETC-206 with 2.5 mg/kg of Dasatinib not only increases tumor growth inhibition in a dose-dependent manner but, more importantly leads to 2, 5, and 8 out of 8 tumor-free animal
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- ETC 206 DataSheet MedChemExpress