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Purity: ≥98%
Epothilone A (also abbreviated as Epo A), similar to paclitaxel in terms of mechanism of action, is also a naturally occurring microtubule-stabilizing macrolide agent (also called mitotic inhibitor or tubulin inhibitor) isolated from the myxobacterium Sorangium cellulosum with potential antineoplastic activity. It acts by inhibiting the polymerization of tubulin. The antiproliferative IC50 value of Epothilone A in HCT-116 cell line is 4.4 nM. It has been found that the SKOV-3 human ovarian cancer cells were susceptible to Epothilone A with IC50 value of 20.4 ± 1.4 nM. The antiproliferative capacity of Epothilone A in SKOV-3 cell line (measured as IC50 after 72 h continuous treatment) was six times greater than that of PTX’s. Besides, Epothilone A induced time coursedependent apoptosis and necrosis.
| ln Vitro |
Epothilone A is a competitive inhibitor that prevents tubulin polymers from binding to [3H] paclitaxel. According to Hanes and Dixon analyses, Epothilone A's apparent Ki value is 1.4 μM and 0.6 μM, respectively[1]. When epothilone A is applied to the human T-24 bladder carcinoma cell line in vitro, it is observed to be highly cytotoxic (IC50=0.05 μM). Based on competition experiments, the binding affinities of paclitaxel and epothilone A to tubulin are of the same order of magnitude. The inhibitory concentration (IC50) of paclitaxel (3.6 μM), epothilone A (2.3 μM), and patupilone (3.3 μM) required to remove 100 nM of (3H) paclitaxel from the tubulin binding site[2].
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| References |
[1]. Kowalski RJ, et al. Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)). J Biol Chem. 1997 Jan 24;272(4):2534-41.
[2]. Cheng KL, et al. Novel microtubule-targeting agents - the epothilones. Biologics. 2008 Dec;2(4):789-811. |
| Molecular Formula |
C26H39NO6S
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| Molecular Weight |
493.66
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| CAS # |
152044-53-6
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| SMILES |
O=C(C(C)(C)[C@@H](O)C1)[ C@H](C)[C@@H](O)[C@@H](C)CCC[C@@]2([H])O[C@@]2([H])C[C@@H](/C(C)=C/C3=CSC(C)=N3)OC1=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.21 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 20.8 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: ≥ 2.08 mg/mL (4.21 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 20.8 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: ≥ 2.08 mg/mL (4.21 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 | 2.0257 mL | 10.1284 mL | 20.2569 mL | |
| 5 mM | 0.4051 mL | 2.0257 mL | 4.0514 mL | |
| 10 mM | 0.2026 mL | 1.0128 mL | 2.0257 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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