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MLN8054
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。
MLN8054图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
MLN8054 是一种有效的、选择性的、可口服的 aurora A 激酶抑制剂,IC50 为 4 nM。

Cell experiment:

MLN8054 is added to human tumor cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 to 0.04 mM. MLN8054 at each dilution is added in triplicate with each replicate on a separate plate. Cells treated with DMSO (n=6 wells per plate; 0.2% final concentration) served as the untreated control. The cells are treated with MLN8054 for 96 h at 37℃ in a humidified cell culture chamber. Cell viability in each cell line is measured by using the Cell Proliferation ELISA, BrdU colorimetric kit[1].

Animal experiment:

Mice: Nude mice bearing HCT-116 tumors are treated orally once per day for 21 consecutive days with either vehicle control or MLN8054 at doses of 3, 10, or 30 mg/kg. Tumor volumes are measured by using a vernier caliper and calculated[1].

产品描述

MLN8054 is a potent of Aurora A kinase (AAK) inhibitor consisting of a benzazepine core scaffold with a fused amino pyrimidine and an aryl carboxylic acid which represents an unprecedented kinase inhibitor framework. The inhibition of MLN8054 towards AAK is ATP-competitive, reversible and selective with an IC50value of 4nM, which is more than 40-fold and 100-fold selective comparing to Aurora B kinase (IC50 = 175 nM) and a range of other kinases respectively. MLN8054 exerts antitumor activity against human tumor xenografts through AAK inhibition, which results in deactivation of Pt288, spindle defects, accumulation of G2/M, and apoptosis-induced cell death in tumor cells.

Reference

[1].Mark G. Manfredi, Jeffery A. Ecsedy, Kristan A. Meetze, Suresh K. Balani, Olga Burenkova. Wei Chen, Katherine M. Galvin, Kara M. Hoar, Jessica J. Huck, Patrick J. LeRoy, Emily T. Ray, Todd B. Sells, Bradley Stringer, Stephen G. Stroud, Tricia J. Vos, Gabriel S. Weatherhead, Deborah R. Wysong, Mengkun Zhang, Joseph B. Bolen, and Christopher F. Claiborne. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of aurora A kinase. PNAS 2007; 104(10): 4106-4111