SNS-314 Mesylate

Catalog No.S8699 Batch:S869901

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Technical Data

Formula

C18H15ClN6OS2.CH4O3S
Molecular Weight 527.04 CAS No. 1146618-41-8
Solubility (25°C)* In vitro DMSO 86 mg/mL (163.17 mM)
Ethanol 1 mg/mL (1.89 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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 and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
Targets
Aurora C [1]
(Cell-free assay)		 Aurora A [1]
(Cell-free assay)		 Aurora B [1]
(Cell-free assay)
3 nM 9 nM 31 nM
In vitro In HCT116 colorectal carcinoma cell line, with intact or depleted p53 protein levels, SNS-314 Mesylate shows enhanced efficacy when administered sequentially with other standard chemotherapeutic agents and the most profound synergies are identified for agents that activate the spindle assembly checkpoint, e.g., docetaxel and vincristine[2]. A recent study shows that SNS-314 Mesylate shows potent antiproliferative activity in HCT116 cells and inhibits soft agar colony formation[3].
In vivo The sequential treatment with SNS-314 Mesylate followed by docetaxel 24 hours later produces a significant 72.5% tumor growth inhibition of HCT116 xenografts, while docetaxel and SNS-314 Mesylate as single agents produce no significant inhibition of HCT116 tumor growth[2]. In the HCT116 human colon cancer xenograft model, administration of 50 and 100 mg/kg SNS-314 Mesylate results a dose-dependent inhibition of histone H3 phosphorylation, indicating effective Aurora-B inhibition in vivo. In addition, HCT116 tumors from animals treated with SNS-314 Mesylate exhibits potent and sustained responses including reduction of phosphorylated histone H3 levels, increased caspase-3 and appearance of increased nuclear size[3].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HCT116 SCR and HCT116 p53 RNAi cells

  • Concentrations

    ~125 nM

  • Incubation Time

    48 h

  • Method

    Viability is measured using the CellTiter-Blue cell viability assay. Cells are treated as described above, although with a 5-day incubation period. Cytotoxicity is determined by measuring intracellular ATP using the CellTiter-Glo Luminescence Cell Viability Assay. Cells are seeded in white 96-well tissue culture plates at a density of 1.5-2 × 103 cells/well, and a serial dilution of SNS-314 is dosed in combination with fixed concentrations of either docetaxel or vincristine for a total of 72 hours. Viability is determined as the ratio between the ATP in treated cells versus control cells. Apoptosis is measured using the caspase-Glo 3/7 system. Cells are plated in white 96-well plates as described above and treated first with SNS-314 for 24 hours, washed with 200 μL of 1× PBS, and fresh medium is added with the second agent for 24 hours.
Animal Study:

[2]
  • Animal Models

    HCT116 cells are injected s.c. into the right flank of nu/nu mice

  • Dosages

    ≤42.5 mg/kg

  • Administration

    Administered via i.p.

Selleck's SNS-314 Mesylate has been cited by 5 publications

Concomitant targeting of FLT3 and BTK overcomes FLT3 inhibitor resistance in acute myeloid leukemia through inhibition of autophagy [ Haematologica, 2022, 10.3324/haematol.2022.280884] PubMed: 36226489
Dual Inhibition of AKT and MEK Pathways Potentiates the Anti-Cancer Effect of Gefitinib in Triple-Negative Breast Cancer Cells [ Cancers (Basel), 2021, 13(6)1205] PubMed: 33801977
A New Quantitative Cell-Based Assay Reveals Unexpected Microtubule Stabilizing Activity of Certain Kinase Inhibitors, Clinically Approved or in the Process of Approval [ Front Pharmacol, 2020, 30;11:543] PubMed: 32425788
Localized Myosin II Activity Regulates Assembly and Plasticity of the Axon Initial Segment. [ Neuron, 2018, 97(3):555-570] PubMed: 29395909
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: 23099978

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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