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Catalog No.
Potent Aurora A/B inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
In stock
In stock
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

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IC50: 44 and 19 nM respectively for Aurora A and B in cancer cells

Ki: 8.0 and 9.2 nM for aurora A and B, respectively

The aurora kinases are a family of serine-threonine kinases that interact with components of the mitotic apparatus and that regulate aspects of centrosome maturation, bipolar spindle assembly, chromosome segregation, and cytokinesis. CYC116 has been discoverd as a novel N-phenyl-4-(thiazol-5-yl) pyrimidin-2-amine aurora kinase inhibitor.

In vitro: The anticancer effects of CYC116 were shown to emanate from cell death following mitotic failure and increased polyploidy as a consequence of cellular inhibition of aurora A and B kinases. Moreover, CYC116 was also assessed against other kinases [1].

In vivo: Preliminary in vivo assessment showed that CYC116 was orally bioavailable and possessed anticancer activity. The mean relative tumor volumes of mice receiving CYC116 at both dose levels were less than those of vehicle-treated mice for the duration of the study period [1].

Clinical trials: CYC116 is currently undergoing evaluation in Phase I clinical trials.

[1] Wang S, Midgley CA, Scaërou F, Grabarek JB, Griffiths G, Jackson W, Kontopidis G, McClue SJ, McInnes C, Meades C, Mezna M, Plater A, Stuart I, Thomas MP, Wood G, Clarke RG, Blake DG, Zheleva DI, Lane DP, Jackson RC, Glover DM, Fischer PM.   Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010;53(11):4367-78.

Chemical Properties

StorageStore at -20°C
Cas No.693228-63-6
Solubility≥18.4 mg/mL in DMSO with gentle warming,insoluble in EtOH,insoluble in H2O
Chemical Name4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine
SDFDownload SDF
Canonical SMILESCC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description CYC116 is a potent inhibitor of Aurora A and B with Ki value of 8 nM and 9.2 nM, respectively.
Targets Aurora A Aurora B        
IC50 8 nM 9.2 nM        

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