Tocopherols
Based on 1 Customer Validation
Tocopherols are orally effective antioxidants and ferroptosis inhibitors. Tocopherols scavenge ROS/RNS, alleviate DNA damage, downregulate cyclin D1/c-Myc/TFF/pS2/PGR in an ER-dependent manner, and inhibit ferroptosis mediated by lipid peroxidation. Tocopherols block the occurrence of ferroptosis in Gpx4-knockout Pfa1 cells, with an EC50 value of 1.0-2.3 μM. Tocopherols inhibit tumor growth. Tocopherols can be used in studies related to estrogen-mediated ER+ breast cancer, oxidative stress-induced carcinogenesis, and ferroptosis regulation.
For research use only. We do not sell to patients.
- Purity: 98.6%
- CAS No.: 1406-66-2
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Storage:Pure form -20°C, 3 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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Tocopherols (10 µM; 1-4 days) downregulate the expression of cyclin D1 and c-Myc in estrogen-induced ER-positive MCF-7 cells, and this antiproliferative activity is ER-dependent[1].
Tocopherols (10 µM; 4 days) downregulate the expression of estrogen-responsive genes in estrogen receptor-positive MCF-7 cells induced by estrogen, and this activity is ER-dependent[1].
Tocopherols (10 µM; 24-48 h) moderately reduce etoposide-induced DNA double-strand breaks in MCF-7 cells, as detected by γ-H2AX foci[1].
Tocopherols (10 µM; 24-48 h) significantly reduce estrogen-induced oxidative DNA damage (detected by 8-oxo-dG levels) in ER-positive MCF-7 cells, and this protective activity is ER-dependent[1].
Tocopherols (10 µM; 24-48 h) significantly reduce estrogen-induced nitrosative stress (measured by nitrotyrosine levels) in ER-positive MCF-7 cells, and this protective activity is ER-dependent[1].
Tocopherols (10 µM; 24-48 h) significantly reduce estrogen-induced DNA double-strand breaks (detected by γ-H2AX foci) in estrogen receptor (ER)-positive MCF-7 cells, and this protective activity is dependent on ER[1].
Tocopherols (1-100 μM; 6 h) inhibit lipid peroxidation of liposomes in cell-free FENIX assays[2].
Tocopherols (0-100 μM; 24-72 h) inhibit ferroptosis induced by RSL3, erastin and BSO in HT-1080 cells, but a concentration higher than 10 μM is required to completely suppress RSL3-induced cell death[2].
Tocopherol (0-100 μM; 24-72 h) inhibits ferroptosis induced by RSL3, erastin and BSO in Pfa1 cells[2].
Tocopherol (0-100 μM; 72 h) prevents Gpx4 knockout-induced ferroptosis in Pfa1 cells, with an EC50 value ranging from 1.0 to 2.3 μM[2].
Tocopherols (48 h) reduce erastin- and BSO-induced LDH release in HT-1080 cells[2].
Tocopherol (1-30 μM; 2 h) inhibits RSL3-induced intracellular lipid peroxidation in HT-1080 cells[2].
Tocopherols (0-500 μM; 72 h) exhibit low cytotoxicity in HT-1080 and Pfa1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ER-positive MCF-7 human breast cancer cells, ER-negative MDA-MB-231 cells
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Concentration:10 µM
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Incubation Time:24 h, 48 h
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Result:Attenuated the estrogen-induced increase in 8-oxo-dG levels by 47% (γ-tocopherol).
Attenuated the estrogen-induced increase in 8-oxo-dG levels by 37% (δ-tocopherol).
Demonstrated a weak inhibitory effect on estrogen-induced 8-oxo-dG levels (α-tocopherol).
Caused no estrogen-induced increase in 8-oxo-dG in ER-negative MDA-MB-231 cells.\nDecreased estrogen-induced nitrotyrosine levels by 48%(γ-tocopherol).
Decreased estrogen-induced nitrotyrosine levels by 52% (δ-tocopherol).
Had no inhibitory effect on estrogen-induced nitrotyrosine levels (α-tocopherol).
Caused no estrogen-induced increase in nitrotyrosine in ER-negative MDA-MB-231 cells.\nDecreased estrogen-induced γ-H2AX focus formation by 67% (α-tocopherol).
Decreased estrogen-induced γ-H2AX focus formation by 60% (γ-tocopherol).
Decreased estrogen-induced γ-H2AX focus formation by 58% (δ-tocopherol).
Caused no estrogen-induced increase in γ-H2AX foci in ER-negative MDA-MB-231 cells.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:10 µM
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Incubation Time:24 h, 48 h
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Result:Decreased etoposide-induced γ-H2AX focus formation by 25%(α-tocopherol).
Decreased etoposide-induced γ-H2AX focus formation by 27%(γ-tocopherol).
Decreased etoposide-induced γ-H2AX focus formation by 26%(δ-tocopherol).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nu/nu (female, 7-8 weeks old, immunodeficient, orthotopic xenograft model)[1]
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Dosage:0.2% α-tocopherol; 0.2% γ-tocopherol; 0.2% δ-tocopherol
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Administration:dietary; daily; 5 weeks
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Result:Reduced final tumor volume by 29% and tumor weight by 20% (α-tocopherol).
Reduced final tumor volume by 45% and tumor weight by 37% (γ-tocopherol).
Reduced final tumor volume by 41% and tumor weight by 39% (δ-tocopherol).
Increased serum α-tocopherol levels from 11.7 µM to 34.1 µM (α-tocopherol group).
Increased serum γ-tocopherol levels from 0.230 µM to 2.523 µM (γ-tocopherol group).
Increased serum δ-tocopherol levels from 0.043 µM to 1.479 µM (δ-tocopherol group).
Showed no difference in body weight among treatment groups.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1406-66-2
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Appearance Liquid (Density: 0.93 g/cm3)
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Color Colorless to light yellow
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SMILES
[Tocopherols]
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Bak MJ, et al. Inhibitory Effects of γ- and δ-Tocopherols on Estrogen-Stimulated Breast Cancer In Vitro and In Vivo. Cancer Prev Res (Phila). 2017 Mar;10(3):188-197. [Content Brief]
[2]. Yang H, et al. Tocotrienols exhibit superior ferroptosis inhibition over tocopherols. Scientific reports. 2026 Jan 07;16(1):4497. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tocopherols Related Classifications
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