VX 680

Cat. No. 5907

VX 680 C23H28N8OS [639089-54-6]

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Alternative 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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Bebbington et al (2009) The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg.Med.Chem.Lett. 19 3586. PMID: 19447622.

Harrington et al (2004) VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat.Med. 10 262. PMID: 14981513.

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Keywords: VX 680, supplier, VX680, MK0457, high, affinity, selective, aurora, kinases, inhibitors, inhibits, AurA, AurB, AurC, Tocris Bioscience, Aurora Kinase Inhibitor products

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