现货，SNS-314，sellreck，美国进口，Aurora Kinase YZ剂，CAS号: 1146618-41-8，目录号 S1154

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]

• 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 Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model Pietro Taverna, Jennifer N. Hogan, et al. Mol Cancer Ther 2009;8:930-939
• SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo Jennifer P. Arbitrario,Brian J. Belmont,et al. Cancer Chemother Pharmacol 2010;65:707–717

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