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Submit ReviewVX 680
Description: High affinity and selective Aurora kinase inhibitor
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
Purity: ≥98% (HPLC)
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree 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 biological activity of the product.
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, VX 680 supplier, VX680, MK0457, high, affinity, selective, aurora, kinases, inhibitors, inhibits, AurA, AurB, AurC, MK, 0457, Tozasertib, Aurora, Kinases, 5907, Tocris Bioscience
Citations for VX 680
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.