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Digitoxin is a potent cardiac glycoside acting as a Na+/K+-ATPase inhibitor (EC50 value: 0.78 μM), with a longer half-life than digoxin.
| ln Vitro |
Digitoxins (4-1000 nM, 24-48 h) have anti-tumor effects in MHCC97H, A549, HCT116, and HeLa cells [3]. Digitoxins (4-100 nM, 24-48 h) interfere with the cell cycle of HeLa cells [3]. Digitoxins (20-500 nM, 48 h) activate HeLa cells in South Africa [3]. Digitoxins (0-80 nM, 72 h) reduce the death rate of PC12 cells [1].
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| ln Vivo |
In mice without skin, digitalisin (1-2 mg/kg, intraperitoneal injection, once day for 19 days) exhibits anti-cancer properties [3]. Digitoxin (0.3–3 μg/kg, injected intraperitoneally once daily for four days in a row)
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: MHCC97H, A549, HCT116 and HeLa Cell Tested Concentrations: 4-1000 nM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Reduces the viability of these cancer cells in a dose and time dependent manner, IC50 value range ranged from 0.075 to 0.395 µM after 24 hrs (hours) of digoxigenin treatment and from 0.028 to 0.077 µM after 48 hrs (hours) of digoxigenin treatment. Cell cycle analysis [3] Cell Types: HeLa Cell Tested Concentrations: 4 nM, 20 nM, 100 nM Incubation Duration: 24 hrs (hours), 36 hrs (hours), 48 hrs (hours) Experimental Results: The G2/M phase cell population increased from 16.27 to 18.36, 23.46 and the concentration was At 20 nM, it was 31.51% at 12, 24 and 36 hrs (hours). At concentrations of 4, 20 and 100 nM, the average cell population in G2/M phase increased from 16.27% to 28.07% within 24 hrs (hours). Dramatically diminished protein expression levels of total CDK1 and phosphorylated CDK1. Apoptosis analysis [3] Cell Types: HeLa Cell Tested Concentrations: 20 nM, 100 nM, 500 nM Incubation Duration: 48 hrs (hours) Experimental Results: Bax expressio |
| Animal Protocol |
Animal/Disease Models: Nude mice carrying HeLa tumor xenografts [3]
Doses: 1 mg/kg, 2 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: diminished tumor volume from 330.71±45.61 mm to 214.56.93±73.25 mm. Strongly increases protein levels of cleaved caspase-3. The number of Ki-67 positive cells diminished. Animal/Disease Models: cotton rat [4] Doses: 0.3 μg/kg, 1 μg/kg, 3 μg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results:Blocked cytokine storm. Cytokine expression is affected to varying degrees. Immune cell density remains intact in virus-infected lungs. |
| References |
[1]. Arispe N, et al. Heart failure drug digitoxin induces calcium uptake into cells by forming transmembrane calcium channels [J]. Proceedings of the National Academy of Sciences, 2008, 105(7): 2610-2615.
[2]. Su C T, Hsu J T A, Hsieh H P, et al. Anti-HSV activity of digitoxin and its possible mechanisms [J]. Antiviral research, 2008, 79(1): 62-70. [3]. Gan H, Qi M, Chan C, et al. Digitoxin inhibits HeLa cell growth through the induction of G2/M cell cycle arrest and apoptosis in vitro and in vivo [J]. International Journal of Oncology, 2020, 57(2): 562-573. [4]. Pollard B S, Blanco J C, Pollard J R. Classical drug digitoxin inhibits influenza cytokine storm, with implications for COVID-19 therapy [J]. in vivo, 2020, 34(6): 3723-3730. [5]. Haux J. Digitoxin is a potential anticancer agent for several types of cancer [J]. Medical hypotheses, 1999, 53(6): 543-548. |
| Molecular Formula |
C41H64O13
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|---|---|
| Molecular Weight |
764.95
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| Exact Mass |
764.4347
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| CAS # |
71-63-6
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| Related CAS # |
Gitoxin;4562-36-1
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| SMILES |
C[C@H]1O[C@](O[C@@H]2[C@@H](C)O[C@](O[C@H]3[C@@H](O)C[C@@](O[C@@H]4C[C@](CC[C@]5([H])[C@]6([H])CC[C@@]7(C)[C@]5(O)CC[C@@H]7C(CO8)=CC8=O)([H])[C@]6(C)CC4)([H])O[C@@H]3C)([H])C[C@@H]2O)([H])C[C@H](O)[C@@H]1O
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| Synonyms |
NSC 7529 NSC-7529 NSC7529 Carditalin EPA Pesticide Chemical Code 097002 Digitoxin
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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 (~130.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.27 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 (3.27 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 (3.27 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 | 1.3073 mL | 6.5364 mL | 13.0727 mL | |
| 5 mM | 0.2615 mL | 1.3073 mL | 2.6145 mL | |
| 10 mM | 0.1307 mL | 0.6536 mL | 1.3073 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.
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