cenisertib

Cenisertib is a water-soluble, synthetic small molecule with potential antineoplastic activity. It acts as an ATP-competitive inhibitor of aurora kinases (A, B, and C), which are serine-threonine kinases crucial for cell division and proliferation. By inhibiting these kinases—often overexpressed in certain cancers—cenisertib disrupts mitotic spindle activity and blocks cell separation, leading to polyploidy and tumor cell death. At low nanomolar concentrations it also inhibits other kinases involved in cancer progression such as Fms-like tyrosine kinase 3 (FLT3) and ABL1 tyrosine-protein kinase (BCR/ABL) (including the T315I mutation), while Janus kinase 2 inhibition occurs at higher concentrations. Preclinical studies have shown potent antitumor effects both as a single agent and in combination therapies for leukemia models. Toxicities are mainly gastrointestinal and hematopoietic[1][2][3][4][5].

Other names

871357-89-0cenisertib benzoate