Description
General description
A cell-permeable triazolylsulfonamido compound that acts a reversible, ATP-competitive kinase inhibitor with selectivities towards Aurora kinases (IC₅₀ = 11 and 15 nM for Aurora-A, Aurora-B, respectively) and Cdk′s (IC₅₀ = 9, 4, and 3 nM for Cdk1/B, Cdk2/A, and Cdk2/E, respectively). Displays antitumor properties both in vitro (IC₅₀ in the range of 112 - 514 nM against various human cancer cell lines) and in a xenograft murine model in vivo (75-100 mg/kg, i.p.).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Aurora Kinase/Cdk
Product competes with ATP.
Reversible: yes
Target IC₅₀: 11 and 15 nM for Aurora-A, Aurora-B, respectively; 9, 4, and 3 nM for Cdk1/B, Cdk2/A, and Cdk2/E, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Emanuel, S., et al. 2005. Cancer Res.65, 9038.
Lin R., et al. 2005. J. Med. Chem.48, 4208.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
