Flumethrin
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.29%
- CAS No.: 69770-45-2
- Formula: C28H22Cl2FNO3
- Molecular Weight:510.38
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Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:MCF-7 human breast carcinoma cells
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Concentration:0.0001-10 μM; 0.1, 1 μM
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Incubation Time:144 h
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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%.
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Cell Line:MCF-7 human breast carcinoma cells
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Concentration:0.1 μM, 1 μM, 10 μM, 100 μM, 200 μM, 500 μM, 1000 μM, 2000 μM
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Incubation Time:24 h
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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.
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Cell Line:MCF-7 human breast carcinoma cells
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Concentration:1 μM, 10 μM, 100 μM, 1000 μM
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Incubation Time:24 h
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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.
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Cell Line:MCF-7 human breast carcinoma cells
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Concentration:1 μM, 10 μM, 100 μM, 1000 μM
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Incubation Time:24 h
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Result:Increased BAX, TP53, and p21CDKN1A mRNA expression at 1000 μM, while decreased BCL2 mRNA expression compared to the control group.
Parmacokinetics
In Vivo
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.
Chemical Information
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CAS No. 69770-45-2
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Appearance Liquid (Density: 1.342±0.06 g/cm3)
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Molecular Weight 510.38
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Formula C28H22Cl2FNO3
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Color Light yellow to yellow
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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
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Synonyms
FCR 2769
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (481 KB)
- English - EN (481 KB)
- Français - FR (481 KB)
- Deutsch - DE (481 KB)
- Norwegian - NO (481 KB)
- Español - ES (481 KB)
- Swedish - SV (481 KB)
- Italian - IT (481 KB)
- Korean - KR (481 KB)
- Portuguese - PT (481 KB)
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Handling Instructions (2659 KB)
References
[1]. Stanneck D, et al. The synergistic action of imidacloprid and flumethrin and their release kinetics from collars applied for ectoparasite control in dogs and cats. Parasit Vectors. 2012;5:73. Published 2012 Apr 12. [Content Brief]
[2]. Kara-Ertekin S, et al. In vitro toxicological assessment of flumethrin's effects on MCF-7 breast cancer cells. Hum Exp Toxicol. 2021;40(12):2165-2177. [Content Brief]
[3]. Qi S, et al. Flumethrin at sublethal concentrations induces stresses in adult honey bees (Apis mellifera L.). Sci Total Environ. 2020;700:134500. [Content Brief]
[4]. Başçi Z, et al. Toxicokinetic of flumethrin in rabbits. Drug Chem Toxicol. 2015;38(1):92-97. [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, 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 |
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| 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 |
Flumethrin Related Classifications
HY-107835 Related Classifications
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