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编 号:F193918
分子式:C18H17ClN2O4S
分子量:392.86
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生物活性:
HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity.

体内研究:
HJC0416 (腹腔注射 10 mg/kg;口服 100 mg/kg;每日一次,持续 7 天) 在小鼠中减少肿瘤生长,体重没有明显减轻。Animal Model:6 weeks, female nude mice (MDA-MB-231 cells)
Dosage:10 mg/kg for i.p.; 100 mg/kg for p.o.
Administration:I.p. or p.o.; daily for 7 days
Result:Decreased the tumor volume for 67% as compared to the control mice for i.p.; the growth of xenograft tumors in mice was also significantly reduced at a dose of 100 mg/kg by 46%.

体外研究:
HJC0416 (0-10 μM; 48 h) 在 MDA-MB-231 细胞中显示抗增殖活性并诱导细胞凋亡。HJC0416 (0-10 μM; 12 h) 降低 p-STAT3 (Tyr-705)、Cyclin D1 的表达并增加cleaved caspase-3 蛋白的表达。
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