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MPI-0479605
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MPI-0479605图片
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
MPI-0479605 是一种有效的、选择性的 ATP 竞争性 Mps1 抑制剂,IC50 为 1.8 nM。

Animal experiment:

HCT-116 or Colo-205 cells are transplanted subcutaneously into the flanks of nude (nu+/nu+) mice and compound (MPI-0479605) treatment is initiated when tumor masses reaches an average size of 100 mm3. MPI-0479605 is formulated in 5% dimethylacetamide (DMA)/12% ethanol/40% PEG-300, ispinesib is formulated in 2% cremaphor/2% DMA, and 5-fluorouracil is formulated in 2% sodium bicarbonate. Tumor volume is measured using vernier calipers and tumor growth inhibition (TGI) is calculated as: %TGI= 100-100(change in median tumor volume of treated)/(change in median tumor volume control)[1].

产品描述

MPI-0479605 is a small-molecule inhibitor of the Mitotic Kinase Mps1 with IC50 value of 1.8nM [1].

MPI-0479605 is a selective and ATP competitive inhibitor of Mps1. It shows no significant inhibition of 120 other kinases. In cells treated with nocodazole, MPI-0479605 inhibits Mps1 function through promoting the degradation of both cyclin B and securing. MPI-0479605 also suppresses the autophosphorylation of Mps1 in HEK293T cells overexpressing this enzyme. In A549 cells during mitosis, MPI-0479605 causes defects in chromosome segregation. It destroys the ability of cells to align chromosomes at the metaphase plate. Besides that, MPI-0479605-treated cells also show a significant delay or arrest in cell-cycle progression. Moreover, treatment of MPI-0479605 leads to a significant decrease in cell viability in HCT-116 cells and finally causes cell death with GI50 values ranging from 30nM to 100nM. Furthermore, MPI-0479605 shows potent antitumor effects in tumor xenograft models. MPI-0479605 at dose of 30mg/kg results in TGI of 49% in mice bearing HCT-116 xenografts [1].

References:
[1] Tardif K D, Rogers A, Cassiano J, et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Molecular cancer therapeutics, 2011, 10(12): 2267-2275.