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 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 639089-54-6 |
| PubChem ID | 5494449 |
| InChI Key | GCIKSSRWRFVXBI-UHFFFAOYSA-N |
| Smiles | CN1CCN(C2=NC(SC3=CC=C(C=C3)NC(C4CC4)=O)=NC(NC5=NNC(C)=C5)=C2)CC1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.46 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 464.59. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.15 mL | 10.76 mL | 21.52 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets
References
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
Keywords: VX 680, supplier, VX680, MK0457, high, affinity, selective, aurora, kinases, inhibitors, inhibits, AurA, AurB, AurC, MK, 0457, Tozasertib, Aurora, Kinases, Aurora, Kinases, Tocris Bioscience
