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Overview
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Background
VX-680 (also known as MK-0457 or tozasertib), discovered through a molecular screening campaign, is a potent inhibitor of pan-aurora kinase as well as other kinases including Src, GSK3β, Flt3, JAK2, BCR-Abl (wild type) and BCR-Abl (T315I mutant). It binds to the inactive conformations of non-aurora kinases preventing activation, which leads to the inhibition of a wide array of kinases. Having been extensively investigated in cell lines and/or xenografts in animal models, VX-680 exhibits high degree of anti-tumor activity against a broad spectrum of tumor types, including ovarian, renal cell carcinoma, thyroid, oral squamous cell, CML (wild-type and mutant BCR-Abl), AML, and MM.
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- Properties
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Overview