Catalog Number: 5907
Alternate Names: MK 0457, Tozasertib
Chemical Name: N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide
Biological Activity
High affinity and selective Aurora kinase inhibitor (Ki values are 0.6, 5 and 18 nM for Aurora A, Aurora C and Aurora B, respectively). Also exhibits affinity for FLT-3 and Abl. Exhibits selectivity for Aurora kinase over 190 other protein kinases. Inhibits proliferation and induces apoptosis in a number of cancer cell lines in vitro. Reduces tumor size in leukemia and colon cancer cell xenografts in mice.
Technical Data
  • M.Wt:
    464.59
  • Formula:
    C23H28N8OS
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    639089-54-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.
    Harrington et al.
    Nat.Med., 2004;10:262
  2. The discovery of the potent aurora inhibitor MK-0457 (VX-680).
    Bebbington et al.
    Bioorg.Med.Chem.Lett., 2009;19:3586

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