VX 680

Pricing Availability Delivery Time Qty
Cat.No. 5907 - VX 680 | C23H28N8OS | CAS No. 639089-54-6
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)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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View all Aurora Kinase Inhibitors

Keywords: VX680 MK0457 high affinity selective aurora kinases inhibitors inhibits AurA AurB AurC MK 0457 Tozasertib Aurora Kinases

Citations for VX 680

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Literature in this Area

Cancer

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

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

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.

Pathways for VX 680

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