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  3. Flumethrin

Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide. Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer.

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Flumethrin

Flumethrin Chemical Structure

CAS No. : 69770-45-2

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Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide. Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer[1][2][3][4].

In Vitro

Flumethrin (10 μM) binds preferentially to the open state of voltage-gated Na+ channels in isolated Spodoptera frugiperda neuronal cells, preventing channel closure only after channel activation by current pulses[1].
Flumethrin (0.000064-5 μg/cm2; 24 h; 48 h), applied as a surface coating, dose-dependently kills adult Ctenocephalides felis fleas in vitro, with 100% mortality achieved at ≥1 μg/cm2 by 48 h and an ED50 of 0.039 μg/cm2 for 48 h mortality[1].
Flumethrin (0.0001-10 μM; 144 h) acts as a partial to full estrogen agonist in MCF-7 human breast carcinoma cells, inducing proliferation with relative proliferative effects of 77% at 0.1 μM and 80% at 1 μM compared to 17β-estradiol[2].
Flumethrin (0.1 μM) upregulates estrogen-responsive genes TFF1, ESR1, and PGR in MCF-7 human breast carcinoma cells, confirming estrogenic activity[2].
Flumethrin (0.1-2000 μM; 24 h) reduces viability of MCF-7 human breast carcinoma cells with an IC50 of 1671 μM after 24 h incubation, and induces significant concentration-dependent cytotoxicity at concentrations of 100 μM and higher[2].
Flumethrin (1-2000 μM; 24 h) induces significant lipid peroxidation in MCF-7 human breast carcinoma cells at concentrations of 1000 μM and higher after 24 h incubation[2].
Flumethrin (1-1000 μM; 24 h) induces concentration-dependent apoptosis in MCF-7 human breast carcinoma cells, with significant increases in late apoptotic cells at 100 μM and 1000 μM after 24 h incubation[2].
Flumethrin (1000 μM; 24 h) induces apoptosis in MCF-7 human breast carcinoma cells via a mitochondrial pathway, upregulating BAX, TP53, and p21CDKN1A and downregulating BCL2 mRNA expression after 24 h incubation[2].
Flumethrin (1-1000 μM; 24 h) induces significant genotoxicity in MCF-7 human breast carcinoma cells at all tested concentrations (1, 10, 100, 1000 μM) after 24 h incubation, increasing MN, NBUD, and NPB frequencies without altering nuclear division index[2].
Flumethrin (1-1000 μM; 24 h) induces significant DNA strand breaks in MCF-7 human breast carcinoma cells at concentrations of 10 μM and higher after 24 h incubation, as measured by increased Olive tail moment, tail moment, tail % DNA, and tail length in the comet assay[2].

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

Cell Proliferation Assay[2]

Cell Line: MCF-7 human breast carcinoma cells
Concentration: 0.0001-10 μM; 0.1, 1 μM
Incubation Time: 144 h
Result: Induced MCF-7 cell proliferation relative to solvent control at 0.1 μM and 1 μM, with relative proliferative effect values of 77% and 80%.

Cell Viability Assay[2]

Cell Line: MCF-7 human breast carcinoma cells
Concentration: 0.1 μM, 1 μM, 10 μM, 100 μM, 200 μM, 500 μM, 1000 μM, 2000 μM
Incubation Time: 24 h
Result: Reduced MCF-7 cell viability in a concentration-dependent manner at 100 μM and higher compared to untreated cells.
Had an IC50 value of 1671 μM for 24 h incubation.

Apoptosis Analysis[2]

Cell Line: MCF-7 human breast carcinoma cells
Concentration: 1 μM, 10 μM, 100 μM, 1000 μM
Incubation Time: 24 h
Result: Triggered concentration-dependent apoptotic morphological changes.
Decreased viable cells to 84.6% at 10 μM; decreased viable cells to 71.8% and increased late apoptotic cells to 19.4% at 100 μM; decreased viable cells to 66.0% and increased late apoptotic cells to 22.6% at 1000 μM compared to the control group.

Real Time qPCR[2]

Cell Line: MCF-7 human breast carcinoma cells
Concentration: 1 μM, 10 μM, 100 μM, 1000 μM
Incubation Time: 24 h
Result: Increased BAX, TP53, and p21CDKN1A mRNA expression at 1000 μM, while decreased BCL2 mRNA expression compared to the control group.
Parmacokinetics
Species Dose Route MRT Vd Vdss V1 CLtotal AUC0-∞ T1/2 (Absorption) Cmax Tmax F
Rabbit[4] 10 mg/kg i.v. 48.0 h 13917 mL/kg 13844 mL/kg 2768 mL/kg 284 mL/h/kg 36.1 mg·h/L / / / /
Rabbit[4] 10 mg/kg p.o. 59.7 h 17369 mL/kg / 9457 mL/kg 458 mL/h/kg 22.0 mg·h/L 1.89 h 0.54 μg/mL 5.42 h 60.9 %
In Vivo

Flumethrin (4.5% by collar weight; 45 mg per 1 g collar; slow-release collar; continuously; up to 240 days) maintains acaricidal efficacy against Rhipicephalus sanguineus ticks for up to 8 months, with 100% overall efficacy observed in dog hair samples at all tested time points and in cat hair samples at 12 hours post-contact[1].
Flumethrin (6.25-100 mg/L; oral; single 4-h exposure) exhibits high acute oral toxicity to newly emerged honey bees, with a 48-h LD50 of 0.47 µg/bee[3].
Flumethrin (0.01-1.0 mg/L; oral; continuous daily; 14 days) induces oxidative stress, detoxification responses, immune dysregulation, and midgut apoptosis in newly emerged honey bees, alongside increased food consumption and low cumulative mortality[3].

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

Molecular Weight

510.38

Formula

C28H22Cl2FNO3

CAS No.
Appearance

Liquid (Density: 1.342±0.06 g/cm3)

Color

Light yellow to yellow

SMILES

N#CC(C1=CC=C(C(OC2=CC=CC=C2)=C1)F)OC(C3C(C3(C)C)/C=C(C4=CC=C(C=C4)Cl)\Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (195.93 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 1.9593 mL 9.7966 mL 19.5932 mL
5 mM 0.3919 mL 1.9593 mL 3.9186 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.90 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 (4.90 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9593 mL 9.7966 mL 19.5932 mL 48.9831 mL
5 mM 0.3919 mL 1.9593 mL 3.9186 mL 9.7966 mL
10 mM 0.1959 mL 0.9797 mL 1.9593 mL 4.8983 mL
15 mM 0.1306 mL 0.6531 mL 1.3062 mL 3.2655 mL
20 mM 0.0980 mL 0.4898 mL 0.9797 mL 2.4492 mL
25 mM 0.0784 mL 0.3919 mL 0.7837 mL 1.9593 mL
30 mM 0.0653 mL 0.3266 mL 0.6531 mL 1.6328 mL
40 mM 0.0490 mL 0.2449 mL 0.4898 mL 1.2246 mL
50 mM 0.0392 mL 0.1959 mL 0.3919 mL 0.9797 mL
60 mM 0.0327 mL 0.1633 mL 0.3266 mL 0.8164 mL
80 mM 0.0245 mL 0.1225 mL 0.2449 mL 0.6123 mL
100 mM 0.0196 mL 0.0980 mL 0.1959 mL 0.4898 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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