Bigelovin
Based on 1 Customer Validation
Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
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- Pureté: 99.92%
- CAS No.: 3668-14-2
- Formule: C17H20O5
- Masse moléculaire:304.34
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | ED50 |
4.9 μM
Compound: Bigelovin
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Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay
Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay
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[PMID: 24959987] |
| HMEC-1 | IC50 |
2679.2 nM
Compound: Bigelovin
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Inhibition of HMEC1 cells growth measured after 48 hrs by MTT assay
Inhibition of HMEC1 cells growth measured after 48 hrs by MTT assay
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[PMID: 23231968] |
| HMEC-1 | IC50 |
946.2 nM
Compound: Bigelovin
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Inhibition of HMEC1 cells growth measured after 48 hrs
Inhibition of HMEC1 cells growth measured after 48 hrs
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[PMID: 23231968] |
| MCF-10A | IC50 |
26 μM
Compound: 14
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Cytotoxicity against human MCF10A cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MCF10A cells assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 24044895] |
| MCF7 | IC50 |
2.1 μM
Compound: 14
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Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 24044895] |
| MDA-MB-231 | IC50 |
2.3 μM
Compound: 14
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Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 24044895] |
| RAW264.7 | IC50 |
0.9 μM
Compound: 13
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Antiinflammatory action in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 30 mins before LPS challenge measured after 24 hrs by griess reaction
Antiinflammatory action in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 30 mins before LPS challenge measured after 24 hrs by griess reaction
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[PMID: 21894898] |
In Vitro
Bigelovin (0-20 μM, 24-72 h) significantly inhibits cell viability of liver cancer cells and induces apoptosis and autophagy[1].
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Bigelovin causes a significant increase of p62, LC3B-II, Beclin-1 and a corresponding decrease of p62 levels in a time-dependent manner[1].
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Bigelovin induces cell death involves the suppression of mTOR pathway regulated by ROS production[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and SMMC-7721 cells.
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Concentration:0-20 μM.
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Incubation Time:24, 48, 72 h.
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Result:Significantly reduced the cell viability of HepG2 and SMMC-7721 cells in a dose- and time dependent manner.
No significant difference observed in cell viability of normal liver cell lines, LO2 and LX2, after BigV treatment for 24, 48 or 72 h.
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Cell Line:HepG2 and SMMC-7721 cells.
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Concentration:0-10 μM.
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Incubation Time:24 h.
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Result:The expression of Bcl-2 was decreased, whereas Bax was increased after treatment with BigV. Moreover, Caspase-9, -3 and PARP cleavage were activated significantly after BigV treatment.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HepG2 xenograft model based on the male athymic BALB/c nude mice (5-6 weeks old, 18-22 g)[1].
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Dosage:5, 10, 20 mg/kg.
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Administration:Intravenous injection every 2 days.
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Result:The tumor growth rate was significantly slower in BigV treated groups in a dose-dependent manner, along with the reduced tumor weight.
No significant alteration of body weight and hepatic enzyme levels (AST, ALT and LDH) in serum was observed after BigV administration.
Western blot findings of tumor tissues indicated the activation of apoptosis and autophagy characterized by the increase of cleaved Caspase-3 and PARP, as well as LC3BII levels.
The inactivation of mTOR was also observed in tumor tissues isolated from BigV-treated mice.
Chemical Information
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CAS No. 3668-14-2
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Appearance Solid
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Masse moléculaire 304.34
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Formule C17H20O5
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Color White to off-white
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SMILES
C[C@@]12C(C=C[C@]1([C@@H](C[C@]3([C@H]([C@@H]2OC(C)=O)C(C(O3)=O)=C)[H])C)[H])=O
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (328.58 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). 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 (8.21 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.21 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 | 3.2858 mL | 16.4290 mL | 32.8580 mL | 82.1450 mL |
| 5 mM | 0.6572 mL | 3.2858 mL | 6.5716 mL | 16.4290 mL | |
| 10 mM | 0.3286 mL | 1.6429 mL | 3.2858 mL | 8.2145 mL | |
| 15 mM | 0.2191 mL | 1.0953 mL | 2.1905 mL | 5.4763 mL | |
| 20 mM | 0.1643 mL | 0.8214 mL | 1.6429 mL | 4.1072 mL | |
| 25 mM | 0.1314 mL | 0.6572 mL | 1.3143 mL | 3.2858 mL | |
| 30 mM | 0.1095 mL | 0.5476 mL | 1.0953 mL | 2.7382 mL | |
| 40 mM | 0.0821 mL | 0.4107 mL | 0.8214 mL | 2.0536 mL | |
| 50 mM | 0.0657 mL | 0.3286 mL | 0.6572 mL | 1.6429 mL | |
| 60 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3691 mL | |
| 80 mM | 0.0411 mL | 0.2054 mL | 0.4107 mL | 1.0268 mL | |
| 100 mM | 0.0329 mL | 0.1643 mL | 0.3286 mL | 0.8214 mL |
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