Rafoxanide
Based on 7 publication(s) in Google Scholar
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.
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- Pureza: 98.60%
- No. CAS: 22662-39-1
- Fòrmula: C19H11Cl2I2NO3
- Peso molecular:626.01
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Rafoxanide
More- Acta Pharm Sin B. 2025 Mar;15(3):1535-1551. [Abstract]
- Cell Death Dis. 2026 Apr 10;17(1):465. [Abstract]
- Int J Mol Sci. 2022 Oct 11;23(20):12100. [Abstract]
- Exp Cell Res. 2019 Dec 15;385(2):111691. [Abstract]
- Drug Repurposing. 2026 Jan 30.
- bioRxiv. 2025 March 01.
- L’UNIVERSITE GRENOBLE ALPES. 2021 Apr 13.
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Actividad biológica
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Schistosome |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | CC50 |
>100 μM
Compound: Rafoxanide
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Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay
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[PMID: 30392371] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116
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Concentration:1.25, 2.5, 5μM
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Incubation Time:24 h
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Result:Increased phosphorylate eIF2α and CHOP, which is the hallmark feature of ERS.
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Cell Line:HCEC-1CT, HCT-116 and DLD-1
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Concentration:1.25, 2.5, 5μM
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Incubation Time:24, 48, 60 h
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Result:Detected cell death of HCT-116 and DLD-1 from 48 h while no significant cell death was observed in HCEC-1CT. Pre-incubation of CRC cells with the pan-caspase inhibitor Q-VD-OPH totally reverted the rafoxanide-induced cell death, indicating the involvement of apoptotic pathways.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AOM induced Apcmin/+ mice[3]
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Dosage:7.5 mg/kg
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Administration:Intraperitoneal injection (i.p.), once every 2 d for 88d
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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.
Chemical Information
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No. CAS 22662-39-1
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Appearance Solid
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Peso molecular 626.01
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Fòrmula C19H11Cl2I2NO3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(OC2=CC=C(Cl)C=C2)C(Cl)=C1)C3=CC(I)=CC(I)=C3O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
2025 Mar;15(3):1535-1551. PMID: 40370558 -
Cell Death Dis
2026 Apr 10;17(1):465. PMID: 41963301 -
Int J Mol Sci
WNK1-OSR1 Signaling Regulates Angiogenesis-Mediated Metastasis towards Developing a Combinatorial Anti-Cancer Strategy. [Abstract]2022 Oct 11;23(20):12100. PMID: 36292952 -
Exp Cell Res
Rafoxanide promotes apoptosis and autophagy of gastric cancer cells by suppressing PI3K /Akt/mTOR pathway. [Abstract]2019 Dec 15;385(2):111691. PMID: 31678170 -
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Solvente y solubilidad
DMSO : ≥ 31 mg/mL (49.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. El-Banna HA, et, al. Comparative pharmacokinetics of ivermectin alone and a novel formulation of ivermectin and rafoxanide in calves and sheep. Parasitol Res. 2008 May;102(6):1337-42. [Content Brief]
[2]. van Wyk JA, et, al. Two field strains of Haemonchus contortus resistant to rafoxanide. Onderstepoort J Vet Res. 1987 Jun;54(2):143-6. [Content Brief]
[3]. Laudisi F, et al. Induction of endoplasmic reticulum stress and inhibition of colon carcinogenesis by the anti-helmintic drug rafoxanide. Cancer Lett. 2019;462:1-11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5974 mL | 7.9871 mL | 15.9742 mL | 39.9355 mL |
| 5 mM | 0.3195 mL | 1.5974 mL | 3.1948 mL | 7.9871 mL | |
| 10 mM | 0.1597 mL | 0.7987 mL | 1.5974 mL | 3.9935 mL | |
| 15 mM | 0.1065 mL | 0.5325 mL | 1.0649 mL | 2.6624 mL | |
| 20 mM | 0.0799 mL | 0.3994 mL | 0.7987 mL | 1.9968 mL | |
| 25 mM | 0.0639 mL | 0.3195 mL | 0.6390 mL | 1.5974 mL | |
| 30 mM | 0.0532 mL | 0.2662 mL | 0.5325 mL | 1.3312 mL | |
| 40 mM | 0.0399 mL | 0.1997 mL | 0.3994 mL | 0.9984 mL |
Rafoxanide Related Classifications
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