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Purity: ≥98%
Epothilone B (formerly known as EO-906; patupilone; EPO 906A; EPO906, Patupilone) is a paclitaxel-class of microtubule-stabilizing agent (also called mitotic inhibitor or tubulin inhibitor) with potential antitumor activity and has been approved for cancer treatment. It inhibits the polymerization of tubulin with an EC0.01 of 1.8 μM. It is a nturally occurring compound isolated from the myxobacterium Sorangium cellulosum. Similar to paclitaxel, epothilone B induces microtubule polymerization and stabilizes microtubules against depolymerization conditions. More importantly, in cell culture, Epothilone B is active against paclitaxel-resistant cell lines that express P-glycoprotein. Furthermore, Epothilone B has better water solubility than paclitaxel which eliminates the use of toxic solubilizers such as Cremophor which is used to solubilize paclitaxel and can cause hypersensitivity reactions in patients.
| ln Vitro |
In the HCT-116 cell line cytotoxicity experiment, epothilone B inhibits HCT116 cells with an IC50 of 0.8 nM[1]. An medication that targets microtubules (MT) is called epothilone B, or patupilone. Epothilone B effectively reduces cell growth with an IC50 of 6 nM after 72 hours of treatment, as demonstrated by the MTT cell proliferation experiment, but values ≤1 nM are not cytotoxic. At the non-cytotoxic concentration of 1 nM, epothilone B considerably inhibits transwell cell migration; at 10 nM, the impact is more pronounced[2]. In human medulloblastoma cell lines, epothilone B (Patupilone) is a novel, non-taxane-related, and nonneurotoxic microtubule-stabilizing drug. With an IC50 of 0.53 nM in the D341 cell line, 0.37 nM in the D425Med cell line, and 0.19 nM in the DAOY cell line, epothilone B decreases the proliferative activity in these three cell lines. Epothilone B's effect on clonogenic survival in the D341Med cell line is observed at doses (IC50, 0.50-0.75 nM) that are comparable to the degree of proliferative activity and viability. Nevertheless, at a 10-fold lower concentration of Epothilone B (IC50, 30 pM), the clonogenicity of D425Med and DAOY cells is already significantly decreased. Overall, these findings show that epothilone B has a strong anti-medulloblastoma cell line effect[3].
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| ln Vivo |
In contrast, combined treatment exerts a strong supra-additive tumor growth control, with complete tumor regression in the follow-up period (P<0.005, for ionizing radiation or Epothilone B alone vs combined treatment). Treatment with Epothilone B (Patupilone) or ionizing radiation alone results in a partial tumor growth suppression over 10 days[3].
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| References |
[1]. Regueiro-Ren A, et al. Synthesis and biological activity of novel epothilone aziridines. Org Lett. 2001 Aug 23;3(17):2693-6.
[2]. Pagano A, et al. Epothilone B inhibits migration of glioblastoma cells by inducing microtubule catastrophes and affecting EB1 accumulation at microtubule plus ends. Biochem Pharmacol. 2012 Aug 15;84(4):432-43. [3]. Oehler C, et al. The microtubule stabilizer patupilone (epothilone B) is a potent radiosensitizer in medulloblastoma cells. Neuro Oncol. 2011 Sep;13(9):1000-10 |
| Molecular Formula |
C27H41NO6S
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| Molecular Weight |
507.68
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| CAS # |
152044-54-7
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| Related CAS # |
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| SMILES |
S1C(C([H])([H])[H])=NC(=C1[H])/C(/[H])=C(\C([H])([H])[H])/[C@]1([H])C([H])([H])[C@@]2([H])[C@@](C([H])([H])[H])(C([H])([H])C([H])([H])C([H])([H])[C@]([H])(C([H])([H])[H])[C@@]([H])([C@@]([H])(C([H])([H])[H])C(C(C([H])([H])[H])(C([H])([H])[H])[C@]([H])(C([H])([H])C(=O)O1)O[H])=O)O[H])O2
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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 (4.10 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 (4.10 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 (4.10 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% Propylene glycol :5 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9697 mL | 9.8487 mL | 19.6974 mL | |
| 5 mM | 0.3939 mL | 1.9697 mL | 3.9395 mL | |
| 10 mM | 0.1970 mL | 0.9849 mL | 1.9697 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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