• Catalog Number:

  E1KS1154

• Amount:

  2mg1​ PHYSICAL AND CHEMICAL PROPERTIES

• Storage/Stability:

  at -20℃ 2 years

2​ Biological Activity SNS-314 Mesylate is an ATP-competitive, potent and selective inhibitor of Aurora kinases A (IC50=9.0nM), B (IC50=31nM), and C (IC50=3.4nM). SNS-314 demonstrated remarkable specificity and was found to inhibit only 24 of 219 kinases by 65% greater than that of screening at 1 µM. Histone H3 phosphorylation was potently inhibited by SNS-314 in all 6 cell lines tested with IC50 values ranging from 9 nM in HCT116 cellsto 60 nM in Calu-6 cells .[1,5] SNS-314 Mesylate also displayed significant anti-tumor activity in mouse xenograft models of human breast (MDA-MB-231), prostate (PC-3), lung (H1299 and Calu-6), ovarian (A2780) carcinomas and melanoma (A375). [2,5] SNS-314 Mesylate represents a new class of highly potent Aurora kinase inhibitors and is being evaluated in a phase-1 dose escalation study designed to assess safety and tolerability in patients with advanced solid malignancies. [3,4] 3​ References: Discovery of a potent and selective Aurora kinase inhibitor Johan D. Oslob,Michael J. Romanowski,et al. Bioorg. Med. Chem. Lett. 2008;18:4880–4884 Water-soluble prodrugs of an Aurora kinase inhibitor Johan D. Oslob ,Stacey A. Heumann,et al. Bioorg. Med. Chem. Lett 2009;19:1409–1412 2-Aminobenzimidazoles as potent Aurora kinase inhibitors Min Zhong,Minna Bui,et al. Bioorg. Med. Chem. Lett. 2009;19:5158–5161 The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.