现货,MLN8054 ,CAS号:869363-13-3,美国进口,HDAC-HSP-Aurora , Aurora Kinase , Aurora Kinase 抑制剂,selleck,S1100

信号转导通路: HDAC-HSP-Aurora >> Aurora Kinase >> Aurora Kinase 抑制剂 >> MLN8054http://www.selleck.cn/mln8054-S1100.html

技术数据:

分子量(MW): 476.86

化学式:

C25H15ClF2N4O2

 

溶解度: DMSO ≥95mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >97%

稳定性: at -20℃ 2 years

CAS号: 869363-13-3

生物活性

 

 

MLN8054 is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity[1] .

MLN8054 inhibits recombinant Aurora A kinase activity in vitro and is selective for Aurora A (IC50 = 0.004 μM)over the family member Aurora B (IC50 = 0.172 μM)in cultured cells[2]. MLN8054 treatment results in G2/M accumulation and spindle defects and inhibits proliferation in multiple cultured human tumor cells lines (IC50 0.11-0.86μM) [2] . Growth of human tumor xenografts in nude mice was dramatically inhibited after oral administration of MLN8054 at well tolerated doses[2] .

 

 

 

参考文献

MLN8054, a Small-Molecule Inhibitor of Aurora A, Causes Spindle Pole and Chromosome Congression Defects Leading to Aneuploidy Kara Hoar,Arijit Chakravarty,et al. MOL.CELL.BIOL. June 2007;27:4513–4525

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase Mark G. Manfredi,Jeffrey A. Ecsedy,et al. PNAS March 6, 2007;104:4106–4111

 

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