CYC-116

• CAT Number: I004604
• CAS Number: 693228-63-6
• Molecular Formula: C₁₈H₂₀N₆OS
• Molecular Weight: 368.46
• Purity: ≥95%
• Synonyms: 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine
• Target: Aurora Kinase
• Solubility: DMSO ≥22mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: 3 years -20C powder
• IC50: 8.0 nM(Aurora A); 9.2 nM(Aurora B)
• InChI: InChI=1S/C18H20N6OS/c1-12-16(26-17(19)21-12)15-6-7-20-18(23-15)22-13-2-4-14(5-3-13)24-8-10-25-11-9-24/h2-7H,8-11H2,1H3,(H2,19,21)(H,20,22,23)
• InChIKey: GPSZYOIFQZPWEJ-UHFFFAOYSA-N
• SMILES: CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4

CYC116（Cat No.:I004604）is a highly potent inhibitor of Aurora A and Aurora B kinases, with Ki values of 8.0nM and 9.2nM, respectively. It also exhibits moderate inhibitory activity against VEGFR2 (Ki of 44nM). Interestingly, CYC116 is approximately 50 times more potent against Aurora kinases than CDKs. It does not show inhibitory effects on PKA, Akt/PKB, PKC, GSK-3α/β, CK2, Plk1, and SAPK2A. These specific inhibitory properties make CYC116 a promising candidate for targeted therapies against diseases involving the aberrant activity of Aurora kinases, particularly in cancer treatment.

Reference

[1]. Wang, Shudong et al. Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine Aurora Kinase Inhibitors. Journal of Medicinal Chemistry (2010), 53(11), 4367-4378
[2]. Kamei H, Jackson RC, Zheleva D, Davidson FA.An integrated pharmacokinetic-pharmacodynamic model for an Aurora kinase inhibitor.J Pharmacokinet Pharmacodyn. 2010 Aug;37(4):407-34. Epub 2010 Aug 8.
[3]. Wang S, Midgley CA, Sca?rou 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 Jun 10;53(11):4367-78.