1. Anti-infection Metabolic Enzyme/Protease Cytoskeleton Cell Cycle/DNA Damage
  2. Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic
  3. Fenbendazole

Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53.

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Fenbendazole Chemical Structure

Fenbendazole Chemical Structure

CAS No. : 43210-67-9

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10 mM * 1 mL in DMSO
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Based on 5 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1].

Cellular Effect
Cell Line Type Value Description References
Hepatocyte IC50
3 x 104 nM
Compound: Fenbendazole
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
[PMID: 18212104]
HepG2 EC50
10 μM
Compound: Fenbendazole
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
HepG2 EC50
4 μM
Compound: Fenbendazole
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
PC-3M EC50
2.6 μM
Compound: Fenbendazole
Cytotoxicity against human PC3M cells assessed as reduction in cell viability after 48 hrs by cyquant reagent based fluorescence spectrometric assay
Cytotoxicity against human PC3M cells assessed as reduction in cell viability after 48 hrs by cyquant reagent based fluorescence spectrometric assay
[PMID: 29288939]
In Vitro

Fenbendazole (1 uM; for 24 h) significantly reduces cell growth in tumour cell lines with wild-type p53, H460 and A549 human NSCLC cell lines[1].
Fenbendazole (1 uM; for 24 h) induces apoptosis and causes an increased level of p53 protein in the mitochondrial fraction[1].
Fenbendazole (1 uM; for 24 h) causes cell cycle arrest in the mitotic phase in human NSCLC cells[1].
Fenbendazole (1 uM; for 24 h) causes a partial alteration of the microtubule network in human non small cell lung carcinoma (NSCLC) A549 cells[1].

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

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 1 uM
Incubation Time: For 24 h
Result: Caused an early elevation of cyclin B1/CDK1 levels (8 h as compared to 16 h in case of control untreated cells).
p-histone H3 (Ser10) was found to be up-regulated at 12 and 24 h.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 1 uM
Incubation Time: 8, 16, 24, 32, 40, 48 h
Result: The number of apoptotic cells increased in a time dependent manner with simultaneous decrease in cyclin B1 levels, and ~30% cells had undergone apoptosis after 32 h.

Western Blot Analysis[1]

Cell Line: H460 cells
Concentration: 1 uM
Incubation Time: For 24 h
Result: Caused an increased level of p53 protein in the mitochondrial fraction.
In Vivo

Fenbendazole (1 mg; orally; every second day for 12 day) leads to a marked reduction in tumour size and weight[1].

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

Animal Model: Female athymic nu/nu mice were xenografted with A549 cells[1]
Dosage: 1 mg/mouse
Administration: Orally; every second day for 12 day
Result: Led to a marked reduction in tumour size and weight.
Led to a reduction in hemoglobin content in tumors signifying reduced tumor vascularity.
Molecular Weight

299.35

Formula

C15H13N3O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC)NC1=NC2=CC=C(SC3=CC=CC=C3)C=C2N1

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 : 10 mg/mL (33.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3406 mL 16.7029 mL 33.4057 mL
5 mM 0.6681 mL 3.3406 mL 6.6811 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (3.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 1 mg/mL (3.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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(per animal)

g

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(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:
%
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+
%
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%
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: 99.84%

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 3.3406 mL 16.7029 mL 33.4057 mL 83.5143 mL
5 mM 0.6681 mL 3.3406 mL 6.6811 mL 16.7029 mL
10 mM 0.3341 mL 1.6703 mL 3.3406 mL 8.3514 mL
15 mM 0.2227 mL 1.1135 mL 2.2270 mL 5.5676 mL
20 mM 0.1670 mL 0.8351 mL 1.6703 mL 4.1757 mL
25 mM 0.1336 mL 0.6681 mL 1.3362 mL 3.3406 mL
30 mM 0.1114 mL 0.5568 mL 1.1135 mL 2.7838 mL
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  • 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.

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Fenbendazole
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HY-B0413
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