C188-9

一种STAT3抑制剂；能够结合到STAT3的SH2结构域（Ki=136nM），并抑制G-CSF诱导的患者来源急性髓系白血病（AML）细胞中STAT3的激活（IC50=8-18µM）；在患者来源的AML细胞中诱导细胞凋亡（EC50=6-50µM）；降低HepG2、Huh7和PLC/PRF/5肝癌细胞的活性（IC50分别为10.19µM、11.27µM和11.83µM）；在小鼠中，以100mg/kg的剂量给药，可减少肝脏中Pten基因缺失诱导的肝大泡性和小泡性脂肪变性，从而降低肝细胞癌的发生；在小鼠Lewis肺癌模型中，以12.5mg/kg的剂量给药，可增加肌肉纤维的大小。A STAT3 inhibitor; binds to the STAT3 SH2 domain (Ki = 136 nM) and inhibits G-CSF-induced activation of STAT3 in patient-derived AML cells (IC50s = 8-18 µM); induces apoptosis in patient-derived AML cells (EC50s = 6-50 µM); reduces viability of HepG2, Huh7, and PLC/PRF/5 hepatoma cells (IC50s = 10.19, 11.27, and 11.83 µM, respectively); reduces hepatic Pten deletion-induced hepatic macro- and microsteatosis which reduces the development of hepatocellular carcinomas in mice at 100 mg/kg; increases muscle fiber size in a murine Lewis lung carcinoma model of cancer cachexia at 12.5 mg/kg.分子式C27H21NO5S分子量471.5OC1=C(C2=C(O)C(C=CC=C3)=C3C(NS(C4=CC=C(OC)C=C4)(=O)=O)=C2)C(C=CC=C5)=C5C=C1