Rafoxanide

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^[1][2][3]. In Vitro:Rafoxanide (1.25-5 μM, 24 h) inhibits ERK activation of HT-29 cells and proliferation of HT-29, HCT-116 and DLD-1 in a dose-dependent fashion while doesn't significantly affect the proliferation of the human normal colon epithelial cell lines HCEC-1CT and NCM460^[3].
Rafoxanide (1.25-5 μM, 24 h) blocks HCT-116 and DLD-1 at G0/G1 phase while down-regulating the level of cyclin D1 through inducing ERS^[3].
Rafoxanide (1.25-5 μM, 48 h) activates programmed cell death of HCT-116 and DLD-1^[3].
In Vivo:Rafoxanide (7.5 mg/kg, i.p., once every 2 d for 88d) reduces colonic tumorgenesis in Apc^min/+ mice^[3].