4-(5-Amino-1-(2,6-difluorobenzoyl)-1H-[1,2,4]triazol-3-ylamino)-benzenesulfonamide White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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.). Purity: ≥97% by HPLC. CAS 443797-96-4. Ref.: Emanuel, S., et al. 2005. Cancer Res. 65, 9038. Lin R., et al. 2005. J. Med. Chem. 48, 4208. |
