Epothilone B

Research use only, not for human use.

A blood-brain barrier-permeable microtubule-stabilizing agent that promotes tubulin polymerization and induces G2-M cell cycle arrest with EC50 of 32 nM in HeLa cells.

A blood-brain barrier-permeable microtubule-stabilizing agent that promotes tubulin polymerization and induces G2-M cell cycle arrest with EC50 of 32 nM in HeLa cells; exhibits potent cytotoxicity in MCF-7 and A549 cells (EC50=0.3 and 2.7 nM respectively), and inhibits growth of HCT-15 tumors in mice in vivo; decreases scarring after rodent spinal cord injury by abrogating polarization and directed migration of scar-forming fibroblasts.(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).

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.

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).

EPO-906 | Patupilone

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Tubulin

Cancer

——

152044-54-7

507.6825

C27H41NO6S

>98% (HPLC)

10 mM in DMSO

C/C([C@@H](OC(C[C@H](O)C1(C)C)=O)C[C@H](O2)[C@@]2(C)CCC[C@H](C)[C@H](O)[C@@H](C)C1=O)=C\C3=CSC(C)=N3

4,17-Dioxabicyclo[14.1.0]heptadecane-5,9-dione, 7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(1E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-, (1S,3S,7S,10R,11S,12S,16R)-

(-20℃)

With Ice Pack

≥ 2 years