SNS-314/SNS314

SNS-314/SNS314

SNS-314/SNS314

编号ABP000119 化学名称SNS-314/SNS314 CAS1057249-41-8 MDL: MFCD16621142 分子式C18H15ClN6OS2.CH4O3S 分子量527.048 纯度 >99%

化学名称 : SNS-314/SNS314

CAS : 1057249-41-8

英文名称: SNS-314/SNS314

英文同义词: SNS-314 MESYLATE

溶解度:Soluble in DMSO

储存条件:Storage at -20C 2 years

生物活性

SNS-314 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 greater than 65% when screened at 1uM. 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.SNS-314 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).SNS-314 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.

参考文献

1.Oslob JD, et al. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4880-4. 2.Oslob JD, et al.Bioorg Med Chem Lett. 2009 Mar 1;19(5):1409-12. 3. Zhong M, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5158-61. 4.VanderPorten EC, et al. Mol Cancer Ther. 2009 Apr;8(4):930-9. 5.Arbitrario JP, et al.Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.

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