SNS-314 Mesylate

SNS-314 Mesylate

Catalog Number:
L002369033APE
Mfr. No.:
APE-A4121
Price:
$274
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      • Overview
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          Background

          SNS-314 is an ATP-competitive and selective inhibitor of aurora kinases with IC50 values of 9 nM, 31 nM and 3 nM against Aurora A, Aurora B and Aurora C, respectively [1 and 2].Aurora kinases are serine/threonine kinases that regulate mitosis of cells. They are found to be associated with the onset and propagation of cancer and over-expressed in various tumor cell lines such as melanoma, ovarian, colon, pancreatic and breast tumors. Therefore, aurora kinases are being evaluated as potential targets in cancer therapy .As a potent inhibitor of aurora kinase, SNS-314inhibited proliferation in a broad panel of tumor cell lines and showed potent anti-tumor activity in mice bearing HCT116 xenografts. Besides that, a mechanism of its action was found to be inhibiting the phosphorylation of histoneH3 at Ser10 [1 and 2]. In the FRET-based biochemical assay, SNS-314inhibited Aurora A, B and C with IC50 values of 9, 31 and 3 nM, respectively. When tested against a panel of 219 kinases, SNS-314 only inhibited 24 kinases of them by 65% or above. It suggested that SNS-314 was a selective inhibitor of aurora kinase. In cell-based assays, SNS-314 blocked the proliferation of cancer cells with IC50 value in the range from 1.8 nM (A2780) to 24 nM (HT29). In HCT-116 cells, SNS-314 treatment for 16 hours resulted in distinct cell-cycle defects [2]. In human tumor xenograft mouse models, administration of SNS-314 exerted significant anti-tumor activities against xenografts of PC-3, H1299, A2780, MDA-MB-231 and A375 cells. The TGI value achieved between 54% and 91% when the dose was 170 mg/kg. The administration also caused a profound and sustained inhibition of pHH3 which was a substrate of Aurora B [2].

          [1] Oslob J D, Romanowski M J, Allen D A, et al. Discovery of a potent and selective aurora kinase inhibitor. Bioorganic & medicinal chemistry letters, 2008, 18(17): 4880-4884.
          [2] Arbitrario J P, Belmont B J, Evanchik M J, et al. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer chemotherapy and pharmacology, 2010, 65(4): 707-717.

      • Properties
        • Alternative Name
          1-(3-chlorophenyl)-3-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-1,3-thiazol-2-yl]urea;methanesulfonic acid
          CAS Number
          1146618-41-8
          Molecular Formula
          C18H15ClN6OS2·CH4O3S
          Molecular Weight
          527.04
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥26.35 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

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