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Biological Activity:
An Aurora kinase inhibitor, used to treat patients with advanced solid tumors.An orally-active inhibitor of Aurora kinases A and B, and VEGFR2, currently in clinical trial for cancer treatment.CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
References:
Carlson, H., et al.: Mol. Pharmacol., 57, 213 (2000), Hou, T., et al.: Curr. Pharm. Des., 10, 1011 (2004), Verdonk, M., et al.: J. Med. Chem., 48, 6504 (2005)