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Epothilone B

CAS No. : 152044-54-7

MCE 国际站：Epothilone B

产品活性：Epothilone B是微管稳定剂，K_i 为0.71 μM。 它通过与αβ-微管蛋白异二聚体亚基结合而起作用，导致αβ-微管蛋白解离的减少。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Anti-infection  |  Apoptosis

作用靶点：Microtubule/Tubulin  |  Fungal  |  Apoptosis  |  Antibiotic  |  Bacterial

In Vitro: Epothilone B inhibits HCT116 cells with IC₅₀ of 0.8 nM in HCT-116 cell line cytotoxicity assay. 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. 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.

In Vivo: 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).

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