CYC-116 is a potent Aurora kinase inhibitor exhibiting Ki values of 8.0 and 9.2 nM for Aurora kinases A and B, respectively. It is significantly less potent against a panel of cyclin-dependent kinases and other related kinases, with the exception of Flt-3 (Ki = 44 nM). CYC-116 exhibits broad-spectrum...

CYC-116 inhibits aurora kinases B and C (AurB, AurC), preventing mitotic spindle formation and proper completion of mitosis. This compound exhibits anticancer chemotherapeutic activity and is currently in clinical trials. CYC-116 inhibits proliferation in a variety of in vitro cancer models.

Soluble in DMSO or ethanol. CYC116 is an orally active small molecule multi-kinase inhibitor with anti-neoplastic activity. CYC116 inhibits Aurora kinases A/B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis....

Description: 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-3alpha/beta, CK2, Plk1 and SAPK2A. Phase 1. Target: FLT, CDK, Aurora Kinase, VEGFR, S6 Kinase....