PF-03814735

PF-03814735 is a novel, potent, orally bioavailable small molecule that acts as a reversible ATP-competitive inhibitor of Aurora kinase A and Aurora kinase B. These serine/threonine kinases are essential for mitotic checkpoint control during cell division. By inhibiting Aurora A and B kinases (with IC50 values in the low nanomolar range), PF-03814735 disrupts phosphorylation events critical for chromosome segregation and cytokinesis. This results in inhibition of cellular proliferation and the formation of polyploid multinucleated cells. The drug has demonstrated antitumor activity in preclinical models and was evaluated in phase I clinical trials for advanced solid tumors but development was discontinued. Sensitivity to the drug correlates with certain genetic backgrounds such as Myc gene family status and retinoblastoma pathway members[1][3][4][5][6].

Other names

N-(2-((1S,4R)-6-((4-(Cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1,2,3,4-tetrahydro-1,4-epiminonaphthalen-9-yl)-2-oxoethyl)acetamide