1. Anti-infection Cytoskeleton Cell Cycle/DNA Damage Stem Cell/Wnt JAK/STAT Signaling Apoptosis Autophagy
  2. Parasite Microtubule/Tubulin STAT MDM-2/p53 Apoptosis Autophagy
  3. Flubendazole

Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites.

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

Flubendazole Chemical Structure

Flubendazole Chemical Structure

CAS No. : 31430-15-6

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Based on 6 publication(s) in Google Scholar

Other Forms of Flubendazole:

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Description

Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites[1][2].

IC50 & Target[1][2]

STAT3

 

In Vitro

Flubendazole (0-400 μM; 48 h) inhibits human colorectal cancer (CRC) cells proliferation[1].
Flubendazole (0.3-1.2 μM; 48 h) induces apoptosis in CRC cells[1].
Flubendazole (0.3-1.2 μM; 24 h) induces autophagy initiation by inactivating mTOR and P62, and upregulating LC3-I/II in CRC cells[1].
Flubendazole (0.3-1.2 μM; 24 h) strongly reduces the expression of P-STAT3 in a dose and time-dependent manner[1].

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

Cell Viability Assay[1]

Cell Line: CRC cells (HCT116, RKO and SW480)
Concentration: 0-400 μM
Incubation Time: 48 h
Result: Effectively reduces the viability of CRC cells (HCT116, RKO and SW480) in a concentration-dependent manner, with an IC50 of 2-5 μM.

Apoptosis Analysis[1]

Cell Line: CRC cells (HCT116, RKO and SW480)
Concentration: 0.3, 0.6, 1.2 μM
Incubation Time: 48 h
Result: Increased the proportion of apoptotic cells in a dose-dependent manner.
Dose-dependently effectively increases caspase-3 activity.

Cell Autophagy Assay[1]

Cell Line: CRC cells (HCT116, RKO and SW480)
Concentration: 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
Result: Induced autophagy initiation by inactivating mTOR and P62, and upregulating LC3-I/II, which are classical marker of autophagy.

Western Blot Analysis[1]

Cell Line: CRC cells (HCT116, RKO and SW480)
Concentration: 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
Result: Strongly reduced the expression of phosphorylated STAT3 (P-STAT3) in a dose and time-dependent manner.
No obvious change in total STAT3 expression.
Decreased expression of MCL1 and survivin in a dose-dependent manner.
In Vivo

Flubendazole (10, 30 mg/kg; i.p; every other day; 14 days) inhibits growth of CRC tumor xenografts[1].

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

Animal Model: Female BALB/c athymic nude mice (6-8 weeks) with HCT116 cells[1]
Dosage: 10  or 30 mg/kg
Administration: Intraperitoneal injection; every other day; 14 days
Result: Markedly reduced the tumor volume.
Significantly reduces the protein level of P-STAT3, promotes autophagy and induces apoptosis in vivo.
Molecular Weight

313.28

Formula

C16H12FN3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC)NC1=NC2=CC=C(C(C3=CC=C(F)C=C3)=O)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 : 4.17 mg/mL (13.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1920 mL 15.9602 mL 31.9203 mL
5 mM 0.6384 mL 3.1920 mL 6.3841 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.

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 5 mg/mL (15.96 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.33%

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 3.1920 mL 15.9602 mL 31.9203 mL 79.8008 mL
5 mM 0.6384 mL 3.1920 mL 6.3841 mL 15.9602 mL
10 mM 0.3192 mL 1.5960 mL 3.1920 mL 7.9801 mL
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    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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Flubendazole
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HY-B0294
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