2. Metabolic Enzyme/Protease Anti-infection MAPK/ERK Pathway Apoptosis
  3. Oxidative Phosphorylation Parasite p38 MAPK Raf Apoptosis
  4. 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.

For research use only. We do not sell to patients.

Rafoxanide Chemical Structure

Rafoxanide Chemical Structure

CAS No. : 22662-39-1

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Rafoxanide:

Rafoxanide Related Antibodies

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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BRaf c-Raf Raf

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

Schistosome

 

Cellular Effect
Cell Line Type Value Description References
HEK293 CC50
> 100 μM
Compound: Rafoxanide
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
[PMID: 30392371]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rafoxanide Related Antibodies

Western Blot Analysis[3]

Cell Line: HCT-116
Concentration: 1.25, 2.5, 5μM
Incubation Time: 24 h
Result: Increased phosphorylate eIF2α and CHOP, which is the hallmark feature of ERS.

Apoptosis Analysis[3]

Cell Line: HCEC-1CT, HCT-116 and DLD-1
Concentration: 1.25, 2.5, 5μM
Incubation Time: 24, 48, 60 h
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.
In Vivo

Rafoxanide (7.5 mg/kg, i.p., once every 2 d for 88d) reduces colonic tumorgenesis in Apcmin/+ mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: AOM induced Apcmin/+ mice[3]
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.
Molecular Weight

626.01

Formula

C19H11Cl2I2NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(OC2=CC=C(Cl)C=C2)C(Cl)=C1)C3=CC(I)=CC(I)=C3O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5974 mL 7.9871 mL 15.9742 mL
5 mM 0.3195 mL 1.5974 mL 3.1948 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 98.60%

SDS (392 KB)

COA (246 KB) RP-HPLC (95 KB)

Handling Instructions (2659 KB)
References

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
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Rafoxanide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rafoxanide22662-39-1Oxidative PhosphorylationParasitep38 MAPKRafApoptosisRaf kinaseshalogenated salicylanilineantiparasiticHemonchusFasciolaEstrus ovisenergy metabolismuncoupling oxidative phosphorylationBRAF V600Ecolorectal cancerApcmin/+ miceHCEC-1CTHCT-116DLD-1HT-29Inhibitorinhibitorinhibit

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