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CDK&Aurora kinase

SNS-314 Mesylate (1146618-41-8)

SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.

Not Intended for Therapeutic Use. For research use only.

CAS: 1146618-41-8 Category

SNS-314 Mesylate (1146618-41-8) Description

SNS-314 is a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.

SNS-314 blocks proliferation in a broad panel of tumor cell lines (HCT116, A2780, PC-3, HeLa, MDA-MB-231, H-1299, and HT29) with IC50 values ranging from 1.8 nM in A2780 ovarian cancer cells to 24 nM in HT29 colon cancer cells. In the HCT116 human colon cancer xenograft model, administration of 50 and 100 mg/kg SNS-314 leads to dose-dependent inhibition of histone H3 phosphorylation for at least 10 h. SNS-314 shows significant tumor growth inhibition in a dose dependent manner under a variety of dosing schedules including weekly, bi-weekly, and 5 days on/9 days off.

 

SNS-314 Mesylate (1146618-41-8) Specifications

Product Name SNS-314 Mesylate
Synonyms SNS314; SNS-314; SNS 314; SNS-314 mesylate
Chemical Names N-(3-Chlorophenyl)-N’-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea mesylate
Purity ≥98% (HPLC)
CAS Number  1146618-41-8
Molecular Formula C19H19ClN6O4S3
Molecular Weight 527.03
Monoisotopic Mass 526.032 g/mol
MDL number N/A
InChIKey FYCODPVDEFFWSR-UHFFFAOYSA-N
InChi Code InChI=1S/C18H15ClN6OS2.CH4O3S/c19-11-2-1-3-12(8-11)24-17(26)25-18-21-9-13(28-18)4-6-20-16-15-14(5-7-27-15)22-10-23-16;1-5(2,3)4/h1-3,5,7-10H,4,6H2,(H,20,22,23)(H2,21,24,25,26);1H3,(H,2,3,4)
SMILES O=C(NC1=NC=C(CCNC2=C3C(C=CS3)=NC=N2)S1)NC4=CC=CC(Cl)=C4.OS(=O)(C)=O
Form Powder
Color Light yellow solid
Solubility  Soluble in DMSO (>50 mg/ml)
Storage Temp.  −20°C
Shelf life >2 years if stored properly
Handling Protect from air and light
Application A potent and selective inhibit

 

 

RIDADR NONH for all modes of transport

References:

[1].  Liu F, Wang G, Wang X, Che Z, Dong W, Guo X, Wang Z, Chen P, Hou D, Zhang Q, Zhang W, Pan Y, Yang D, Liu H. Targeting high Aurora kinases expression as an innovative therapy for hepatocellular carcinoma. Oncotarget. 2017 Apr 25;8(17):27953-27965. doi: 10.18632/oncotarget.15853. PubMed PMID: 28427193; PubMed Central PMCID: PMC5438621.

[2].  Quagliariello V, Armenia E, Aurilio C, Rosso F, Clemente O, de Sena G, Barbarisi M, Barbarisi A. New Treatment of Medullary and Papillary Human Thyroid Cancer: Biological Effects of Hyaluronic Acid Hydrogel Loaded With Quercetin Alone or in Combination to an Inhibitor of Aurora Kinase. J Cell Physiol. 2016 Aug;231(8):1784-95. doi: 10.1002/jcp.25283. Epub 2016 Feb 2. PubMed PMID: 26660542.

[3]. Sarvagalla S, Coumar MS. Structural Biology Insight for the Design of Sub-type Selective Aurora Kinase Inhibitors. Curr Cancer Drug Targets. 2015;15(5):375-93. Review. PubMed PMID: 25895501.

[4]. Cheung CH, Sarvagalla S, Lee JY, Huang YC, Coumar MS. Aurora kinase inhibitor patents and agents in clinical testing: an update (2011 – 2013). Expert Opin Ther Pat. 2014 Sep;24(9):1021-38. doi: 10.1517/13543776.2014.931374. Epub 2014 Jun 26. Review. PubMed PMID: 24965505.

[5]. Baldini E, Sorrenti S, D’Armiento E, Guaitoli E, Morrone S, D’Andrea V, Gnessi L, Moretti C, Antonelli A, Catania A, De Antoni E, Ulisse S. Effects of the Aurora kinases pan-inhibitor SNS-314 mesylate on anaplastic thyroid cancer derived cell lines. Clin Ter. 2012;163(5):e307-13. PubMed PMID: 23099978.