产品描述

K858是一种新型的、有效的Eg5抑制剂，抑制Eg5的ATPase活性，IC50为1.3 μM，对Eg5的选择性是对其他驱动蛋白的至少150倍。

靶点（IC50 & Targe）

Eg5 ATPase

体外研究

K858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. Long-term continuous treatment of cancer cells with K858 resulted in antiproliferative effects through the induction of mitotic cell death, and polyploidization followed by senescence. In contrast, treatment of nontransformed cells with K858 resulted in mitotic slippage without cell death, and cell cycle arrest in G1 phase in a tetraploid state. K858 has minimal effects on abnormalities in the number and structure of chromosomes. K858 has no effect on microtubule polymerization in cell-free and cell-based assays[1].

体内研究

K858 exhibits potent antitumor activity in xenograft models of cancer, and induces the accumulation of mitotic cells with monopolar spindles in tumor tissues. K858 is not neurotoxic in a motor coordination test in mice[1].

细胞实验

Cell lines: HCT116 cells

Concentrations: 3 μM

Incubation Time: 18 h

Method:HCT116 cells are treated with vehicle, paclitaxel, vincristine, K858, or monastrol for 18 h.

(Only for Reference)

动物实验

Animal Models: BALB/cAJcl-nu mice inoculated with A2780 cells

Formulation: 0.5% methylcellulose 400

Dosages: 150 and 50 mg/kg

Administration: oral

(Only for Reference)

参考文献

[1] Nakai R, et al. Cancer Res. 2009, 69(9):3901-9.