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MLN8054Aurora A inhibitor

MLN8054

Catalog No. A4114
Size Price Stock Qty
5mg $110.00 In stock
10mg $190.00 In stock
50mg $590.00 In stock
200mg $1,490.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

MLN8054

Biological Activity

Description MLN8054 is an oral, ATP-competitive, selective small-molecule inhibitor of Aurora A with IC50 value of 4 nM.
Targets Aurora A          
IC50 4 nM          

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Chemical Properties

Cas No. 869363-13-3 SDF Download SDF
Chemical Name 4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid
Canonical SMILES C1C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)C(=N1)C4=C(C=CC=C4F)F)NC5=CC=C(C=C5)C(=O)O
Formula C25H15ClF2N4O2 M.Wt 476.86
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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 IC50 value 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

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