Rotenolone
Based on 1 Customer Validation
Rotenolone is a metabolite of Rotenone (HY-B1756), inhibitor of Mitochondrial complex I, and antiproliferative agent, with an IC50 of 137 nM against bovine complex I. Rotenolone undergoes biotransformation via multiple cytochrome P450 isoenzymes in rainbow trout liver microsomes. Rotenolone exhibits anticancer activity against ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, and colon cancer. Rotenolone can be used in studies related to ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, and colon cancer.
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- Pureza : 97.0%
- No. CAS: 509-96-6
- Fòrmula: C23H22O7
- Peso molecular:410.42
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 697 | IC50 |
0.5 μM
Compound: 7
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Cytotoxicity against human 697 cells after 72 hrs by MTS assay
Cytotoxicity against human 697 cells after 72 hrs by MTS assay
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[PMID: 23895019] |
| 697 | IC50 |
0.7 μM
Compound: 7
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Cytotoxicity against human 697 cells after 48 hrs by MTS assay
Cytotoxicity against human 697 cells after 48 hrs by MTS assay
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[PMID: 23895019] |
| A2780 | IC50 |
0.5 μg/mL
Compound: 6
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Cytotoxicity against human A2780 cells
Cytotoxicity against human A2780 cells
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[PMID: 15043430] |
| A2780 | IC50 |
0.95 μM
Compound: 5
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Antiproliferative activity against human A2780 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human A2780 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 20804165] |
| BT-549 | IC50 |
1.6 μM
Compound: 5
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Antiproliferative activity against human BT549 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human BT549 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 20804165] |
| DU-145 | IC50 |
2.7 μM
Compound: 5
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Antiproliferative activity against human DU145 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human DU145 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 20804165] |
| HCC 2998 | IC50 |
2.9 μM
Compound: 5
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Antiproliferative activity against human HCC2998 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human HCC2998 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 20804165] |
| HCT-116 | IC50 |
0.055 ug
Compound: 6
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Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting
Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting
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[PMID: 21452840] |
| HCT-116 | IC50 |
0.055 μg
Compound: 6
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Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting
Cytotoxicity against human HCT116 cells measured per disk after 5 days by hemocytometer counting
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[PMID: 21452840] |
| HT-29 | IC50 |
0.1 μM
Compound: 7
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Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
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[PMID: 23895019] |
| NCI-H460 | IC50 |
2 μM
Compound: 5
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Antiproliferative activity against human NCI-H460 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human NCI-H460 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 20804165] |
| Raji | IC50 |
2.4 μM
Compound: 7
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Cytotoxicity against human Raji cells after 72 hrs by MTS assay
Cytotoxicity against human Raji cells after 72 hrs by MTS assay
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[PMID: 23895019] |
| Raji | IC50 |
5.6 μM
Compound: 7
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Cytotoxicity against human Raji cells after 48 hrs by MTS assay
Cytotoxicity against human Raji cells after 48 hrs by MTS assay
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[PMID: 23895019] |
| U-937 | IC50 |
0.07 μM
Compound: 4, 12a-hydroxyrotenone
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Antiproliferative activity against human U937 cells after 48 hrs by WST-8 assay
Antiproliferative activity against human U937 cells after 48 hrs by WST-8 assay
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[PMID: 17158054] |
| U-937 | IC50 |
0.09 μM
Compound: 4, 12a-hydroxyrotenone
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Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay
Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay
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[PMID: 17158054] |
| U-937 | IC50 |
3.6 μM
Compound: 4, 12a-hydroxyrotenone
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Antiproliferative activity against human U937 cells after 24 hrs by WST-8 assay
Antiproliferative activity against human U937 cells after 24 hrs by WST-8 assay
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[PMID: 17158054] |
In Vitro
Rotenolone potently inhibits proliferation of A2780 human ovarian cancer cells with an IC50 of 0.95 μM[2].
Rotenolone inhibits proliferation of BT-549 human breast cancer, DU 145 human prostate cancer, NCI-H460 human NSCLC, and HCC-2998 human colon cancer cells with IC50 values of 1.6 μM, 2.7 μM, 2.0 μM, and 2.9 μM, respectively[2].
Rotenolone inhibits bovine heart mitochondrial complex I with an IC50 of 137 nM[3].
Rotenolone is selectively cytotoxic to LNCaP prostate cancer cells with an ED50 of 0.3-0.7 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 509-96-6
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Appearance Solid
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Peso molecular 410.42
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Fòrmula C23H22O7
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Color White to off-white
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SMILES
O=C1[C@@]2([C@]([H])(OC3=C1C=CC4=C3C[C@@H](O4)C(C)=C)COC5=C2C=C(C(OC)=C5)OC)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (243.65 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.09 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 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.
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.
Protocolo
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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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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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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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[2]. Harinantenaina L, et al. Antiproliferative compounds from Pongamiopsis pervilleana from the Madagascar Dry Forest. J Nat Prod. 2010;73(9):1559-1562. [Content Brief]
[3]. Russell DA, et al. Hydroxylated Rotenoids Selectively Inhibit the Proliferation of Prostate Cancer Cells. J Nat Prod. 2020;83(6):1829-1845. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4365 mL | 12.1826 mL | 24.3653 mL | 60.9132 mL |
| 5 mM | 0.4873 mL | 2.4365 mL | 4.8731 mL | 12.1826 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4365 mL | 6.0913 mL | |
| 15 mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 4.0609 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2183 mL | 3.0457 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4365 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0304 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5228 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4873 mL | 1.2183 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6091 mL |
Rotenolone Related Classifications
HY-119694 Related Classifications
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Keywords
- Rotenolone
- 509-96-6
- Drug Metabolite
- Mitochondrial Metabolism
- Cytochrome P450
- LNCaP prostate cancer cells
- A2780 human ovarian cancer cells
- cytochrome P450 isozymes
- BT-549 human breast cancer cells
- NCI-H460 human NSCLC cells
- mitochondrial complex I
- HCC-2998 human colon cancer cells
- DU 145 human prostate cancer cells
- bovine heart mitochondrial complex I
- rainbow trout hepatic microsomes
- Inhibitor
- inhibitor
- inhibit