Art. -Nr.: HY-13719

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Oleandrin

(Synonyms: PBI-05204)

6 Cited Publications

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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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Reinheit: 99.91%
CAS. Nr.: 465-16-7
Formel: C₃₂H₄₈O₉
Molecular Weight:576.72

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Oleandrin Chemical Structure

CAS. Nr.: 465-16-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Oleandrin (PBI-05204) inhibits the Na⁺, K⁺-ATPase activity with an IC₅₀ of 620 nM.

IC₅₀ & Target

IC50: 620 nM (Na⁺, K⁺-ATPase)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
BJ	IC₅₀	0.026 μM Compound: 1	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	[PMID: 31325787]
BJ	IC₅₀	0.026 μM Compound: 1	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	[PMID: 32645647]
CCRF-CEM	IC₅₀	0.019 μM Compound: 1	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	[PMID: 31325787]
CCRF-CEM	IC₅₀	0.019 μM Compound: 1	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	[PMID: 32645647]
HCT-116	IC₅₀	0.08 μM Compound: 4	Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method	[PMID: 19894733]
HEK293	IC₅₀	28 nM Compound: 1	Cytotoxicity against HEK293 cells after 72 hrs by fluorescence assay Cytotoxicity against HEK293 cells after 72 hrs by fluorescence assay	[PMID: 29693393]
HeLa	IC₅₀	0.062 μM Compound: 1	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	[PMID: 31325787]
HeLa	IC₅₀	0.062 μM Compound: 1	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	[PMID: 32645647]
HPBALL	IC₅₀	14 nM Compound: 1	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	[PMID: 29693393]
HT-29	IC₅₀	0.44 μM Compound: 4	Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method	[PMID: 19894733]
MCF7	IC₅₀	0.033 μM Compound: 1	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	[PMID: 31325787]
MCF7	IC₅₀	0.033 μM Compound: 1	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	[PMID: 32645647]

In Vitro

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.

In Vivo

The effect of Oleandrin is investigated on glioma growth in vivo. To this aim, SCID or C57BL/6 mice are transplanted, respectively, with human U87MG (5×10⁴), U251, GBM19 (5×10⁵), or murine (syngeneic) GL261 (7.5×10⁴) cells into the right striatum and, after 10 d, treated daily with intraperitoneal Oleandrin for an additional 7 d. Oleandrin significantly reduces tumor sizes in human and murine glioma cell models in vivo in a dose-dependent way. High concentrations of Oleandrin (3 mg/kg) are fatal in both models, as expected from the known lethal dose for rodents. Doses of Oleandrin below the lethal dose (0.3 mg/kg) significantly increase the survival time from 32.6±1.4 d to 53.8±9.6 d in mice injected with U87MG cells (n=5-11; p<0.01, log-rank test) and from 23.37±1.2 d to 34.38±3.3 d (n=5-11; p<0.01, log rank test) in mice injected with GL261 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 465-16-7
Appearance Solid
Molecular Weight 576.72
Formel C₃₂H₄₈O₉
Color White to off-white
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
Synonyms

PBI-05204
Structure Classification
- Steroids
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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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
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.
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

Comprehensive Metabolite Profile and Cytotoxic Constituents of Cryptolepis decidua. [Abstract]

2026 May 22;89(5):1462-1477. PMID: 42029115

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7339 mL

8.6697 mL

17.3394 mL

5 mM

0.3468 mL

1.7339 mL

3.4679 mL

10 mM

0.1734 mL

0.8670 mL

1.7339 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[2]

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.

Animal Administration^[3]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Oleandrin

6 Cited Publications

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Oleandrin

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Publications Citing Use of MedChemExpress (MCE) Oleandrin

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Oleandrin

Membrane Transporter/Ion Channel Compound Library

Natural Product Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Lipid Compound Library

Traditional Chinese Medicine Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Natural Product Library

Plant-Sourced Natural Product Library

Membrane Protein-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Natural Product Diversity Scaffold Library

RNA Binding Bioactive Compound Library

Mass Spectrometry Natural Product Library

Publications Citing Use of MedChemExpress (MCE) Oleandrin

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Oleandrin Related Classifications

HY-13719 Related Classifications