Signal transducers and activators of transcription (STATs) are a family of transcription factors essential for the pathogenesis of many cancers. STAT3 in particular has been found to be a critical mediator in the pathogenesis of many tumors. C188-9 is a STAT3 inhibitor by inhibiting STAT3 tyrosine phosphorylation. Acute myeloid leukemia (AML) cell lines treated with increasing doses of the C188-9 for 24h and EC50 values of the 7 acute myeloid leukemia cell lines varied between 6 and 8 μM in GDM-1 and Kasumi-1 cells to more than 43 μM in K562 cells. C188-9 inhibited G-CSF-induced Stat3 phosphorylation in a dose-dependent manner, with IC50 values ranging between 8 and 18 μM in primary pediatric AML cells[3]. CC188-9 reduced cell viability of all three Hepatoma cell lines with IC50 values of 11.27, 10.19 and 11.83 μM for Huh7, PLC/PRF/5 and HepG2, respectively. Intraperitoneal injection of C188-9 (100mg/kg) by daily for 4 weeks to hepatocyte-specific Pten deletion (HepPten-) mouse model inhibited tumor growth (249.02 mm3 and 106.48 mm3 for vehicle- and C188-9-treated mice, respectively; p = 0.04)[4].
搜索
