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Etoposide phosphate disodium (BMY-40481 disodium), the phosphate ester prodrug of etoposide, is a potent anti-cancer chemotherapeutic drug, acting as a topoisomerase II inhibitorthat prevents re-ligation of DNA strands.
| ln Vitro |
Position 4' of the etoposide molecule's E ring has a phosphate group, which makes etoposide phosphate disodium a water-soluble derivative and likely prodrug of etoposide[1]. Etoposide phosphate disodium (0-1 μM; 72 hours) has dose-dependent inhibitory effects on HCT116 FBXW+/+, FBXW-/-, and p53-/-, with IC50 values of 0.945 μM, 0.375 μM, and 1.437 μM, respectively[2]. In cells lacking FBXW7, p53 recovery is delayed by etoposide phosphate disodium (25 μM; 6 hours). Furthermore, in FBXW7-/-cells, FBXW7 expression is absent[2].
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| ln Vivo |
On day 8, female CD-1 mice administered with etoposide phosphate (50, 100, or 150 mg/kg in a single dosage) exhibit increasing ataxia, decreased righting reflex, and splaying and paresis of the fore- and hindlimbs[3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: FBXW+/+, FBXW-/- and p53-/- cell Tested Concentrations: 0.025 μM, 0.05 μM, 0.075 μM, 0.1 μM, 0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM, 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited HCT116 FBXW+/+, FBXW-/- and p53-/- cell growth as a concentration manner. Western Blot Analysis[2] Cell Types: HCT116 FBXW7+/+ or FBXW7-/- cells Tested Concentrations: 25 μM Incubation Duration: 6 hrs (hours) Experimental Results: demonstrated that the recovery of p53 levels after DNA damage is mediated by FBXW7. |
| Animal Protocol |
Animal/Disease Models: Female CD-1 mice[3]
Doses: 50, 100, or 150 mg/kg Route of Administration: intravenous (iv) injection; single dose Experimental Results: Observed degeneration of dorsal root ganglion cells and axonal degeneration of their distal and proximal processes in peripheral nerves, dorsal spinal roots, and dorsal funiculi of the spinal cord at all doses under light microscopy (LM). |
| References |
[1]. Witterland AH, et al. Etoposide phosphate, the water soluble prodrug of etoposide. Pharm World Sci. 1996 Oct;18(5):163-70.
[2]. Cui D, et al. FBXW7 Confers Radiation Survival by Targeting p53 for Degradation.Cell Rep. 2020 Jan 14;30(2):497-509.e4. [3]. Bregman CL, et al. Etoposide- and BMY-40481-induced sensory neuropathy in mice.Toxicol Pathol. 1994 Sep-Oct;22(5):528-35. [4]. SUMMARY OF PRODUCT CHARACTERISTICS |
| Molecular Formula |
C₂₉H₃₁NA₂O₁₆P
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|---|---|
| Molecular Weight |
712.50
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| CAS # |
122405-33-8
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| Related CAS # |
Etoposide phosphate;117091-64-2
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| SMILES |
O=C1OC[C@]2([H])[C@H](O[C@@]3([H])[C@@H]([C@@H](O)[C@]4([H])O[C@H](C)OC[C@@]4([H])O3)O)C3C=C4OCOC4=CC=3[C@@H](C3C=C(OC)C(OP(O)(O)=O)=C(OC)C=3)[C@@]12[H].[NaH]
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| Synonyms |
Etoposide phosphate disodium Etoposide phosphate disodium
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4035 mL | 7.0175 mL | 14.0351 mL | |
| 5 mM | 0.2807 mL | 1.4035 mL | 2.8070 mL | |
| 10 mM | 0.1404 mL | 0.7018 mL | 1.4035 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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