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CYC116Potent Aurora A/B inhibitor

CYC116

Catalog No. A4125
Size Price Stock Qty
10mg $80.00 In stock
50mg $260.00 In stock
200mg $680.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

CYC116

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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Chemical Properties

Cas No. 693228-63-6 SDF Download SDF
Chemical Name 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine
Canonical SMILES CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4
Formula C18H20N6OS M.Wt 368.46
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

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.

Reference:
[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.