产品
编 号:F762746
分子式:C29H24F6N4O3
分子量:590.52
产品类型
结构图
CAS No: 2971855-37-3
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产品详情
生物活性:
HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis.
体内研究:
HP590 (oral administration; 25 and 50 mg/kg; once daily; 5 w) inhibits GC growth effectively by inhibiting the STAT3 activation and shows better tolerance in GC xenograft model.Animal Model:BALB/c-nude mice injected with GC cells
Dosage:25 and 50 mg/kg
Administration:Oral administration; 25 and 50 mg/kg; once daily; 5 weeks
Result:Inhibited MKN45 tumor growth in a concentration-dependent manner.Inhibited STAT3 phosphorylation at Tyr705 and Ser727 and reduced the expression of the downstream genes.Inhibited the expression of Ki67 (a proliferation marker).Showed no weight loss during HP590 treatment, and no apparent damage in the major organs of mice.
体外研究:
HP590 (0-40 μM; 72 h) shows anti-proliferative activities to MKN45, AGS, and MGC803 cells.HP590 (0-40 nM; 0-24 h) inhibits STAT3 Tyr705 and Ser727 phosphorylation in GC cells, blocks the expression of STAT3 downstream genes (c-Myc and cyclin D1) in GC cells, reduces IL-6-mediated STAT3 nuclear translocation in MKN45 cells.HP590 (5-20 nM; 48 h) induces gastric cancer cell apoptosis.