189406

Aurora Kinase/Cdk Inhibitor

The Aurora Kinase/Cdk Inhibitor, also referenced under CAS 443797-96-4, controls the biological activity of Aurora Kinase/Cdk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(e): Aurora Kinase/Cdk Inhibitor, 4-(5-Amino-1-(2,6-difluorobenzoyl)-1H-[1,2,4]triazol-3-ylamino)-benzenesulfonamide, JNJ-7706621, Aurora Kinase Inhibitor I
• Empirische Formel (Hill-System): C₁₅H₁₂F₂N₆O₃S · xC₂H₃N
• CAS-Nummer: 443797-96-4
• Molekulargewicht: 394.36
• MDL number: MFCD11100270
• UNSPSC Code: 12352202
• NACRES: NA.54
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• 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

Beschreibung

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)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable