TargetValue STAT3 (in HT29 cells) 1.82 μM STAT3 (in MDA-MB 231 cells) 2.14 μM

STAT3-IN-1 (compound 7d: 10, 20 mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model. Animal Model: Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells. Dosage: 10, 20 mg/kg. Administration: Oral administration once every other day for two weeks. Result: Arrested tumor growth with no obvious body weight loss.

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. Apoptosis Analysis Cell Line: MDA-MB-231 cell lines. Concentration: 0-10 μM. Incubation Time: 48 hours. Result: The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 μM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%. Western Blot Analysis Cell Line: MDA-MB-231 and HT-29 cell lines. Concentration: 0-10 μM. Incubation Time: 48 hours. Result: Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells. Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685.

STAT3-IN-1 (compound 7d) 是一种出色的、选择性的 STAT3 的口服活性抑制剂，在HT29细胞和MDA-MB 231细胞中的IC50值分别为1.82 μM和2.14 μM。STAT3-IN-1 诱导肿瘤细胞凋亡。