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Aurora A inhibitor I

CAS 1158838-45-9

C31H31ClFN7O2  MW 588.07

Purity: 99%

Ordering Information:

Cat. No. Axon 1597       Prime Source 

Qty1: 5 mg (research sample) / €145  $189

Promotion: 2 x 5 mg @ €210  $273

Qty2: 25 mg (research sample) / €510  $663    

Promotion: 2 x 25 mg @ €750  $975

Qty3: on request

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Biological Activity:   Potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.   This ligand has much higher selectivity of Aurora A vs Aurora B than another recently described relatively selective Aurora A inhibitor MLN8054, which shows 43-fold selectivity for Aurora A over Aurora B in enzymatic assays.   References:   I Aliagas-Martin et al. A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J. Med. Chem. 2009, 52(10), 3300-7. [online]   Chemical Name: N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide

Aurora A inhibitor I | Axon Medchem | Axon 1597

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AurA in the spotlight ...

Activation Signal for Aurora-A Oncogene: Discovery May Lead to More Potent Drug Combinations

- ScienceDaily (Sept 7, 2010)

Rapid calcium-dependent activation of Aurora-A kinase

- Nature Comm.  (Sept 7, 2010)