Epothilone B  (Synonyms: EPO 906; Patupilone)

Epothilone B is a microtubule stabilizer with a K_i of 0.71μM. It acts by binding to the αβ-tubulin heterodimer subunit which causes decreasing of αβ-tubulin dissociation.

EC0.01: 1.8 μM (Microtubule/Tubulin)^[1]

Epothilone B inhibits HCT116 cells with IC₅₀ of 0.8 nM in HCT-116 cell line cytotoxicity assay^[1]. Epothilone B (Patupilone) is a microtubule (MT) targeting agent. As shown by MTT cell proliferation assay, after 72 h of treatment Epothilone B efficiently inhibits cell growth with an IC₅₀ of 6 nM, while concentrations ≤1 nM are not cytotoxic. Epothilone B significantly inhibits transwell cell migration at the non-cytotoxic concentration of 1 nM, and the effect is more evident at 10 nM^[2]. Epothilone B (Patupilone) is a novel, non-taxane-related and nonneurotoxic microtubule-stabilizing agent in human medulloblastoma cell lines. Epothilone B reduces the proliferative activity in the D341 cell line, with an IC₅₀ of 0.53 nM; in the D425Med cell line, with an IC₅₀ of 0.37 nM; and in the DAOY cell line, with an IC₅₀ of 0.19 nM. In the D341Med cell line, the effect of Epothilone B on clonogenic survival is at dose range of Epothilone B similar to the level of proliferative activity and viability (IC₅₀, 0.50-0.75 nM). However, the clonogenicity of D425Med and DAOY cells is already strongly reduced at a 10-fold lower concentration of Epothilone B (IC₅₀, 30 pM). These results overall demonstrate that Epothilone B is highly potent against different medulloblastoma cell lines^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Treatment with Epothilone B (Patupilone) or ionizing radiation alone results in a partial tumor growth suppression over 10 days, whereas 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)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

507.68

C₂₇H₄₁NO₆S

152044-54-7

Solid

White to off-white

O=C(C[C@H](O)C1(C)C)O[C@H](/C(C)=C/C2=CSC(C)=N2)C[C@]3([H])O[C@]3(C)CCC[C@H](C)[C@H](O)[C@@H](C)C1=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Regueiro-Ren A, et al. Synthesis and biological activity of novel epothilone aziridines. Org Lett. 2001 Aug 23;3(17):2693-6.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]