Soluble in DMSO or ethanol. In mammals, three Aurora kinases, Aurora A, Aurora B, and Aurora C, are expressed. Aurora C expression is mainly restricted to testis, where it functions during meiosis, whereas Aurora A and B play key functions regulating mitosis. Aurora A is localized to the centrosome and spindle...

Tozasertib (VX680) is an Aurora kinase inhibitor found to suppress tumor growth.

Tozasertib is a potent inhibitor of all aurora kinases, including the A, B and C isotypes (Ki=0.6nM, 18nM and 4.6nM, respectively). It also inhibits ABL kinase (Ki=30nM), an imatinib-resistant ABL mutant (T315I) kinase (Ki=42nM), and Flt-3 (Ki=30nM). Tozasertib binds to an inactive aurora conformation. Solubility:...

The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis. MK-0457 is a potent pan-Aurora kinase inhibitor but...

Description: Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases. Target: Aurora Kinase, Autophagy. Smiles: CN1CCN(CC1)c1cc(Nc2cc(C)[nH]n2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1. References: Harrington EA, et...