SNS-314 Inhibitor CAS No. 1057249-41-8

Cat. No.	Name	Size	Price	Add Cart
KI1458	SNS-314	5 mg	$320

Chemical Characteristic

Product Name	SNS-314
CAS No.	1057249-41-8
Molecular Weight	430.93
Formula	C₁₈H₁₅ClN₆OS₂
Chemical Name	N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea
Smiles	N(C(=O)Nc1sc(cn1)CCNc1c2c(ncn1)ccs2)c1cc(ccc1)Cl
Chemical Structure

Biological activities

SNS-314 is a potent and selective Aurora kinase inhibitor. SNS-314 potently inhibits Aurora A, Aurora B and Aurora C with IC50 of 9, 31, and 3.4 nM, respectively.^[1] Treatment of anaplastic thyroid carcinomas (ATC) derived cell lines (CAL-62, 8305C, 8505C and BHT-101) with SNS-314 inhibits proliferation in a time- and dose-dependent manner, with IC50s ranging from 2.6 to 26.6 nM. SNS-314 treatment prevents the completion of mitosis leading to polyploidy in CAL-62 cells in vitro.^[2] In a HCT116 xenografts model, the sequential treatment with SNS-314 followed by docetaxel produces a significant 72.5% tumor growth inhibition, while SNS-314 alone produces no significant inhibition of HCT116 tumor growth.^[3] In another HCT116 human colon cancer xenograft model, SNS-314 administration (50 and 100 mg/kg) leads to dose-dependent inhibition of histone H3 phosphorylation for at least 10 hours. SNS-314 treatment also shows potent and sustained responses including reduction of phosphorylated histone H3 levels, increased caspase-3 and appearance of increased nuclear size.^[4]

Protocols

In vitro: SNS-314 is dissolved in DMSO.^[5]

References

[1] Oslob JD, et al. Discovery of a potent and selective aurora kinase inhibitor. Bioorg Med Chem Lett. 2008, 18(17): 4880-4884. [2] Baldini E, et al. Effects of the Aurora kinases pan-inhibitor SNS-314 mesylate on anaplastic thyroid cancer derived cell lines. Clin Ter. 2012, 163(5): e307-e313. [3] VanderPorten EC, et al. The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model. Mol Cancer Ther. 2009, 8(4): 930-939. [4] Arbitrario JP, et al. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010, 65(4): 707-717. [5] Deng XQ, et al. Pharmacophore modelling and virtual screening for identification of new Aurora-A kinase inhibitors. Chem Biol Drug Des. 2008, 71(6): 533-539.

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