产品
编 号:F282592
分子式:C19H11Cl2I2NO3
分子量:626.01
产品类型
结构图
CAS No: 22662-39-1
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产品详情
生物活性:
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research.
体内研究:
Rafoxanide (7.5 mg/kg, 静脉注射, 两天一次, 88d) 可减少 Apcmin/+小鼠结肠肿瘤的发生。Animal Model:AOM induced Apcmin/+mice
Dosage:7.5 mg/kg
Administration:Intraperitoneal injection (i.p.), once every 2 d for 88d
Result:Exerted less number and size of AOM induced lesions in the colon. No significant body weight changes were observed. Detected adenomas (28.6%), advanced adenomas (67.8%) and adenocarcinoma (3.6%) in control group as adenomas (33.3%), advanced adenomas (25%%) and no obvious lesions(41.6%) were detected in treated group. Caused increased signal for p-eIF2α, CHOP and cleaved caspase-3 in tumor tissues while these signal in non-tumor colon epithelium were barely detectable.
体外研究:
Rafoxanide (1.25-5 μM, 24 h) 以剂量依赖性方式抑制 HT-29 细胞的 ERK 激活以及 HT-29、HCT-116 和 DLD-1 的增殖,而对人正常结肠上皮细胞 HCEC-1CT 和 NCM460 的增殖无明显影响。Rafoxanide (1.25-5 μM, 24 h) 将 HCT-116 和 DLD-1 细胞阻滞在 G0/G1 期,同时通过诱导内质网应激下调 cyclin D1 水平。Rafoxanide (1.25-5 μM, 48 h) 可激活 HCT-116 和 DLD-1 的程序性细胞死亡。