Oleandrin
Based on 6 publication(s) in Google Scholar
Oleandrin (PBI-05204) inhibits the Na+, K+-ATPase activity with an IC50 of 620 nM.
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- Pureza: 99.91%
- No. CAS: 465-16-7
- Fòrmula: C32H48O9
- Peso molecular:576.72
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) Oleandrin
More- Cell Death Dis. 2021 Mar 24;12(4):314. [Abstract]
- Acta Pharmacol Sin. 2025 Jun;46(6):1733-1741. [Abstract]
- Phytother Res. 2024 Aug;38(8):4151-4167. [Abstract]
- Int Immunopharmacol. 2025 Jan 16:148:114073. [Abstract]
- J Nat Prod. 2026 May 22;89(5):1462-1477. [Abstract]
- Biomed Pharmacother. 2020 Apr;124:109852. [Abstract]
Customer Validation & Images
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WB
Actividad biológica
IC50: 620 nM (Na+, K+-ATPase)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BJ | IC50 |
0.026 μM
Compound: 1
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Cytotoxicity against human BJ cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Cytotoxicity against human BJ cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
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[PMID: 31325787] |
| BJ | IC50 |
0.026 μM
Compound: 1
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Cytotoxicity against human BJ cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
Cytotoxicity against human BJ cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
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[PMID: 32645647] |
| CCRF-CEM | IC50 |
0.019 μM
Compound: 1
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Antiproliferative activity against human CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Antiproliferative activity against human CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
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[PMID: 31325787] |
| CCRF-CEM | IC50 |
0.019 μM
Compound: 1
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Cytotoxicity against human CEM cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
Cytotoxicity against human CEM cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
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[PMID: 32645647] |
| HCT-116 | IC50 |
0.08 μM
Compound: 4
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Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
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[PMID: 19894733] |
| HEK293 | IC50 |
28 nM
Compound: 1
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Cytotoxicity against HEK293 cells after 72 hrs by fluorescence assay
Cytotoxicity against HEK293 cells after 72 hrs by fluorescence assay
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[PMID: 29693393] |
| HeLa | IC50 |
0.062 μM
Compound: 1
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Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
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[PMID: 31325787] |
| HeLa | IC50 |
0.062 μM
Compound: 1
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
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[PMID: 32645647] |
| HPBALL | IC50 |
14 nM
Compound: 1
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Cytotoxicity against human HPBALL cells after 72 hrs by alamar blue dye based fluorescence assay
Cytotoxicity against human HPBALL cells after 72 hrs by alamar blue dye based fluorescence assay
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[PMID: 29693393] |
| HT-29 | IC50 |
0.44 μM
Compound: 4
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Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
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[PMID: 19894733] |
| MCF7 | IC50 |
0.033 μM
Compound: 1
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
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[PMID: 31325787] |
| MCF7 | IC50 |
0.033 μM
Compound: 1
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
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[PMID: 32645647] |
Study of Na,K-ATPase inhibition shows an IC50 (nM) of 620 for Oleandrin. The inhibition of Na,K-ATPase by Oleandrin confirms that it likely exert its toxic effect through inhibition of sodium pump activity[1]. When treated with a series of concentrations of Oleandrin (0.2-25 nM), the undifferentiated CaCO-2 cells are sensitive as evidenced by an IC50 of 8.25 nM. In contrast, a maximum growth inhibition of only 20% is reached in differentiated CaCO-2 cells even though they are treated with Oleandrin concentrations as high as 25 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 465-16-7
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Appearance Solid
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Peso molecular 576.72
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Fòrmula C32H48O9
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Color White to off-white
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SMILES
O=C1OCC([C@H]2[C@@H](OC(C)=O)C[C@]3(O)[C@]4([H])CC[C@]5([H])C[C@@H](O[C@H]6C[C@@H]([C@H]([C@H](C)O6)O)OC)CC[C@]5(C)[C@@]4([H])CC[C@]23C)=C1
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Synonyms
PBI-05204
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Oleandrin, a cardiac glycoside, induces immunogenic cell death via the PERK/elF2α/ATF4/CHOP pathway in breast cancer. [Abstract]2021 Mar 24;12(4):314. PMID: 33762577 -
Acta Pharmacol Sin
Bardoxolone displays potent activity against triple negative breast cancer by inhibiting the TRIP13/STAT3 circuit. [Abstract]2025 Jun;46(6):1733-1741. PMID: 39939802 -
Phytother Res
Oleandrin enhances radiotherapy sensitivity in lung cancer by inhibiting the ATM/ATR-mediated DNA damage response. [Abstract]2024 Aug;38(8):4151-4167. PMID: 39136618 -
Int Immunopharmacol
Oleandrin inhibits osteoclast differentiation by targeting the LRP4/MAPK/NF-κB signalling pathway to treat osteoporosis. [Abstract]2025 Jan 16:148:114073. PMID: 39823799 -
J Nat Prod
2026 May 22;89(5):1462-1477. PMID: 42029115 -
Biomed Pharmacother
Oleandrin induces apoptosis via activating endoplasmic reticulum stress in breast cancer cells. [Abstract]2020 Apr;124:109852. PMID: 31972357
Oleandrin purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Apr;124:109852. [Abstract]
MCF7 and MDA-MB-231 cells are treated with Oleandrin or DMSO for 24 h. The expression of Bcl-2, Bim, and Bax is detected by western blot using β-actin as a loading control.
Solvente y solubilidad
DMSO : 100 mg/mL (173.39 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.33 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 (4.33 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.
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
Undifferentiated wild-type and well-differentiated CaCO-2 cells are treated with a range of concentrations of Oleandrin (0.2-25 nM). After 48 h, cells are labeled with BrdU and relative cell proliferation is determined with a BrdU Cell Proliferation Kit[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
After tumor cell injection, SCID or C57BL/6 mice are monitored daily. The end point is determined by lack of physical activity or death. The mean survival time is calculated using the Kaplan-Meier method and statistical analysis is performed using a log-rank test. For cotreatment with Temozolomide (TMZ), 10 d after tumor injection, mice are treated with Oleandrin (0.03, 0.3, or 3 mg/kg/daily, i.p.), TMZ (50 mg/kg, i.p., every 2 d for a total of 4 times with a stop of 2 weeks) or both. The dosing scheme is chosen starting from these data to be reasonably sure that a constant concentration of drug is maintained along the experiment. Animals used in Kaplan-Meier survival studies receive up to four TMZ cycles.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jortani SA, et al. Inhibition of Na,K-ATPase by oleandrin and oleandrigenin, and their detection by digoxin immunoassays. Clin Chem. 1996 Oct;42(10):1654-8. [Content Brief]
[2]. Yang P, et al. Cellular location and expression of Na+, K+-ATPase α subunits affect the anti-proliferative activity of oleandrin. Mol Carcinog. 2014 Apr;53(4):253-63. [Content Brief]
[3]. Garofalo S, et al. The Glycoside Oleandrin Reduces Glioma Growth with Direct and Indirect Effects on Tumor Cells. J Neurosci. 2017 Apr 5;37(14):3926-3939. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7339 mL | 8.6697 mL | 17.3394 mL | 43.3486 mL |
| 5 mM | 0.3468 mL | 1.7339 mL | 3.4679 mL | 8.6697 mL | |
| 10 mM | 0.1734 mL | 0.8670 mL | 1.7339 mL | 4.3349 mL | |
| 15 mM | 0.1156 mL | 0.5780 mL | 1.1560 mL | 2.8899 mL | |
| 20 mM | 0.0867 mL | 0.4335 mL | 0.8670 mL | 2.1674 mL | |
| 25 mM | 0.0694 mL | 0.3468 mL | 0.6936 mL | 1.7339 mL | |
| 30 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4450 mL | |
| 40 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 50 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8670 mL | |
| 60 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7225 mL | |
| 80 mM | 0.0217 mL | 0.1084 mL | 0.2167 mL | 0.5419 mL | |
| 100 mM | 0.0173 mL | 0.0867 mL | 0.1734 mL | 0.4335 mL |
Oleandrin Related Classifications
HY-13719 Related Classifications
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