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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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ln Vitro |
Studies on Na,K-ATPase inhibition revealed that oleandrin had an IC50 (nM) of 620. Oleandrin's inhibition of Na,K-ATPase indicates that it may impede sodium pump action in order to cause toxicity [1]. Undifferentiated CaCO-2 cells showed sensitivity to oleandrin at doses ranging from 0.2 to 25 nM, with an IC50 of 8.25 nM. In contrast, differentiated CaCO-2 cells could only achieve a maximum growth inhibition of 20% when treated with oleandrin at concentrations as high as 25 nM [2].
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ln Vivo |
Studies were conducted on oleandrin's effects on glioma growth in vivo. Hence, the right striatum of SCID or C57BL/6 mice was transplanted with human U87MG (5×104), U251, GBM19 (5×105), or murine (syngeneic) GL261 (7.5×104) cells, respectively. , and ten days later, oleandrin was administered intraperitoneally every day for seven days. In vivo glioma cell models in mice and humans exhibit a dose-dependent reduction in tumor growth due to oleandrin. High doses of oleandrin (3 mg/kg) were fatal in both models, as would be expected based on the known lethal dose in rodents. The survival time of mice injected with U87MG cells was significantly extended from 32.6±1.4 days to 53.8±9.6 days (n=5-11; p<0.01, log-rank test) by oleandrin doses below the lethal dose (0.3 mg/kg) and from 23.37±1.2 days to 34.38±3.3 days (n=5-11; p<0.01, log-rank test) for mice injected with GL261 cells [3].
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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.
[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. [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 |
Molecular Formula |
C32H48O9
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Molecular Weight |
576.72
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Exact Mass |
576.32983
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CAS # |
465-16-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(O[C@H]1C[C@]2(O)C3CC[C@]4([H])C[C@@H](O[C@H]5C[C@H](OC)[C@@H](O)[C@H](C)O5)CC[C@]4(C)[C@@]3([H])CC[C@]2(C)C1C6=CC(OC6)=O)=O
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Synonyms |
PBI-05204 PBI 05204 PBI05204
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~173.39 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.