Oleandrin (Synonyms: PBI-05204)

Name: Oleandrin
Brand: MedChemExpress
SKU: HY-13719
Rating: 5.0 (4 reviews)

Cat. No.: HY-13719 Purity: 99.93%: FAQs
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Oleandrin (PBI-05204) inhibits the Na⁺, K⁺-ATPase activity with an IC₅₀ of 620 nM.

For research use only. We do not sell to patients.

Oleandrin Chemical Structure

CAS No. : 465-16-7

Size	Price	Stock	Quantity
5 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 798	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1270	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1960	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Based on 4 publication(s) in Google Scholar

Other Forms of Oleandrin:

Oleandrin (Standard) Get quote

3 Publications Citing Use of MCE Oleandrin

: 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.

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Description

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 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]
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]
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]
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]
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	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]
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]
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]
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]
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]

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

Molecular Weight

576.72

Formula

C₃₂H₄₈O₉

CAS No.

465-16-7

Appearance

Solid

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

Structure Classification

Steroids

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.93%

Select Batch:

Data Sheet (281 KB) SDS (584 KB)

COA (252 KB) HNMR (277 KB) LCMS (260 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Oleandrin465-16-7PBI-05204PBI05204PBI 05204Na+/K+ ATPaseSodium potassium pumpInhibitorinhibitorinhibit

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Oleandrin (Synonyms: PBI-05204)

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3 Publications Citing Use of MCE Oleandrin

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Oleandrin Related Antibodies

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Oleandrin Related Classifications

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