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)
| Quality Segment | 100 |
| assay | ≥97% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | DMSO: 15 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | Fc1c(c(ccc1)F)C(=O)N2NC(=NC2=N)Nc3ccc(cc3)[S](=O)(=O)N |
| InChI | 1S/C15H12F2N6O3S/c16-10-2-1-3-11(17)12(10)13(24)23-14(18)21-15(22-23)20-8-4-6-9(7-5-8)27(19,25)26/h1-7H,(H2,19,25,26)(H3,18,20,21,22) |
| InChI key | KDKUVYLMPJIGKA-UHFFFAOYSA-N |
