mln8054

MLN8054 is a selective, orally bioavailable small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase. It acts as an ATP competitive and reversible inhibitor with high selectivity for Aurora A over Aurora B and other kinases. By inhibiting Aurora A kinase, MLN8054 disrupts mitotic spindle assembly and chromosome segregation during cell division, leading to inhibition of cell proliferation and induction of apoptosis in cancer cells. The drug was developed by Millennium Pharmaceuticals (now part of Takeda) and entered Phase I clinical trials for advanced solid tumors including colon, breast, bladder, pancreatic cancers, and other advanced malignancies. Dose-limiting toxicity was primarily reversible somnolence due to off-target effects on the GABA-A receptor alpha1 subunit[1][3][5][6].

Other names

869363-13-34-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid