STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis.IC50 & Target:IC50: 1.82 μM (STAT3 in HT29 cells), 2.14 μM (STAT3 in MDA-MB 231 cells).In Vitro:STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) inhibits the STAT3 acetylation at lysine 685 and affected its specific genes expressions.
STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) induces tumor cells apoptosis in MDA-MB-231 cells.In Vivo:STAT3-IN-1 (compound 7d: 10, 20 mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model.