Danusertib

Soluble in DMSO or ethanol. Aurora kinases are key regulators of protein phosphorylation during mitosis, and these serine/threonine kinases interact with other cellular proteins to help control chromosome assembly and segregation during mitosis. Aurora kinases are often highly expressed in malignancies and solid tumors. Danusertib (PHA-739358) is a small molecule pan- Aurora kinase inhibitor that also has activity against other cancer-relevant kinases such as Bcr-Abl tyrosine kinase. Other off target effects of danusertib include inhibition of receptor tyrosine kinases such as FGFR-1, and TrkA. Danusertib demonstrates nanomolar IC(50) values for the Aurora kinases all under 100nM and it also demonstrates potent anti-proliferation effects in cell proliferation assays with IC(50) values ranging from 20nM for A2780 cells to <200nM. Target: Abl - Aurora A - BCR - FGFR , Kinase Group: Other , Substrate: Serine-Threonine