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Overview
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Background
MK-5108, also known as VX-689, is a novel, potent and selective inhibitor of Aurora A kinase (AAK) that competitively binds to the ATP binding site of AAK and hence potently inhibits the activity of AAK with 50% inhibition concentration IC50 value of 0.064 nM. MK-5108 also inhibits other members of Aurora kinase family, including Aurora B kinase (IC50 = 14 nM) and Aurora C kinase (IC50 = 12 nM), with a lesser potency. MK-5108 has been extensively studies and found to exhibit antitumor activity in a wide range of cancer types, including breast, cervix, colorectal, ovary and pancreas neoplasms.
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- Properties
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Overview