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Rafoxanide

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Chemical Structure| 22662-39-1 同义名 : 雷复尼特 ;NSC 355278;Disalan;Rafoxanida.;EINECS 245-148-9 ; Duofas;BRN 2228187;Bovanide;Flukanide;Ranide
CAS号 : 22662-39-1
货号 : A214599
分子式 : C19H11Cl2I2NO3
纯度 : 99%
分子量 : 626.01
MDL号 : MFCD00682899
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(47.92 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

生物活性
描述 Rafoxanide, a veterinary antihelminthic drug, has shown antibacterial activity in vitro against Gram-positive bacteria. In the murine peritoneal sepsis model with Col-R (colistin-resistant) strains, rafoxanide plus CMS, compared with CMS alone, increased mouse survival to 53.8% and 73.3%, and reduced bacterial loads in tissues and blood between 2.34 and 4.99 log10 cfu/g or mL, respectively[3]. Rafoxanide is commonly used as anti-helminthic medicine in veterinary medicine, a main compound of salicylanilide. Rafoxanide, as an inhibitor of BRAF V600E mutant protein, inhibits the growth of colorectal cancer, multiple myeloma, and skin cancer. Rafoxanide is used in veterinary medicine for the treatment of fascioliasis[4]. Rafoxanide treatment inhibited tumor growth, with no significant side effects, in an MM (multiple myeloma) mouse xenograft model. Combination of rafoxanide with bortezomib or lenalidomide significantly induced synergistic cytotoxicity in MM cells[5]. Rafoxanide was found to exhibit the highest cytotoxic effects (IC50: 1.09 µM for A375 and 1.31 µM for A431 cells). Rafoxanide (40 mg/kg, i.p.) exhibited significant antitumor activity, comparable to that of oxaliplatin (5 mg/kg, i.p.). The combined administration of rafoxanide and oxaliplatin produced a synergistic therapeutic effect[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.60mL

0.32mL

0.16mL

7.99mL

1.60mL

0.80mL

15.97mL

3.19mL

1.60mL
参考文献

[1]Attia AK, Saad AS, et al. Study of Thermal Analysis Behavior of Fenbendazole and Rafoxanide. Adv Pharm Bull. 2017 Jun;7(2):329-334.

[2]Power C, Danaher M, et al. Investigation of the persistence of rafoxanide residues in bovine milk and fate during processing. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2013;30(6):1087-95.

[3]Miró-Canturri A, Ayerbe-Algaba R, Villodres ÁR, Pachón J, Smani Y. Repositioning rafoxanide to treat Gram-negative bacilli infections [published online ahead of print, 2020 Apr 2]. J Antimicrob Chemother. 2020;dkaa103

[4]Liu JZ, Hu YL, Feng Y, et al. Rafoxanide promotes apoptosis and autophagy of gastric cancer cells by suppressing PI3K /Akt/mTOR pathway. Exp Cell Res. 2019;385(2):111691

[5]Xiao W, Xu Z, Chang S, et al. Rafoxanide, an organohalogen drug, triggers apoptosis and cell cycle arrest in multiple myeloma by enhancing DNA damage responses and suppressing the p38 MAPK pathway. Cancer Lett. 2019;444:45‐59

[6]Shi X, Li H, Shi A, et al. Discovery of rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer. Oncol Rep. 2018;40(3):1592‐1600