SNS-314 mesylate
Based on 3 publication(s) in Google Scholar
SNS-314 mesylate is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively.
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- Purity: 99.53%
- CAS No.: 1146618-41-8
- 화학식: C19H19ClN6O4S3
- 분자량:527.04
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) SNS-314 mesylate
MoreAll Aurora Kinase Isoforms
More
Biological Activity
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Aurora A 9 nM (IC50) |
Aurora B 31 nM (IC50) |
Aurora C 6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
<16 nM
Compound: 1c
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Cell cycle arrest in human HCT116 cells assessed as accumulation of 4N DNA by FACS analysis
Cell cycle arrest in human HCT116 cells assessed as accumulation of 4N DNA by FACS analysis
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[PMID: 19646866] |
| HCT-116 | EC50 |
<16 nM
Compound: 21, SNS-314
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Cell cycle arrest in human HCT116 cells assessed as accumulation of 4N DNA phase after 16 hrs by FACS
Cell cycle arrest in human HCT116 cells assessed as accumulation of 4N DNA phase after 16 hrs by FACS
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[PMID: 18678489] |
| HCT-116 | EC50 |
<16 nM
Compound: 21, SNS-314
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Decrease in histone H3 phosphorylation in human HCT116 cells after 16 hrs by Western blot
Decrease in histone H3 phosphorylation in human HCT116 cells after 16 hrs by Western blot
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[PMID: 18678489] |
| HCT-116 | EC50 |
6 nM
Compound: 11, SNS-314
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Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
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[PMID: 19320489] |
| HCT-116 | EC50 |
6 nM
Compound: 1c
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Antiproliferative activity against human HCT116 cells by BrdU incorporation assay
Antiproliferative activity against human HCT116 cells by BrdU incorporation assay
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[PMID: 19646866] |
| HCT-116 | EC50 |
6 nM
Compound: 21, SNS-314
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Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation
Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation
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[PMID: 18678489] |
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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1146618-41-8
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Appearance Solid
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분자량 527.04
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화학식 C19H19ClN6O4S3
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Color White to light yellow
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SMILES
O=C(NC1=CC=CC(Cl)=C1)NC2=NC=C(S2)CCNC3=C4C(C=CS4)=NC=N3.OS(C)(=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Int J Mol Sci
2026 Mar 11;27(6):2587. PMID: 41898448 -
용액&용해도
DMSO : 150 mg/mL (284.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
A homogeneous time-resolved fluorescence (HTRF)-based biochemical IC50 assay is used to test for the kinase activity of the three isoforms of Aurora (A, B, and C) in the presence of SNS-314. A biotin-conjugated histone H3 peptide is used as substrate. Aurora-A kinase (7.5 nM) is assayed in 10 mM Tris–HCl pH 7.2, 10 mM MgCl2, 0.1% BSA, 0.05% Tween 20, 1 mM DTT, 120 nM biotinylated peptide ARTKQTARKSTGGKAPRKQLA-GGK-biotin, 6 μM ATP (2×the Km for the enzyme) for 1 h at 25°C. The reaction is stopped with 200 mM EDTA. Aurora-B and Aurora-C are assayed at 5 nM enzyme concentration, 120 nM biotinylated peptide, and 300 lM ATP (29 the Km for the enzymes) for 1 h at 25°C[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HCT116 cells are treated with various concentrations of SNS-314 for 96 hours. cells are incubated with BrdU for 2 h at 37°C. Cell proliferation activity is evaluated by chemiluminescence detection of BrdU incorporated in DNA[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Tumor mice are treated with vehicle or SNS-314. Animals are weighed, monitored for signs or symptoms of toxic effects, and measured for tumor volumes twice weekly until an end point is met[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Oslob JD, et al. Discovery of a potent and selective aurora kinase inhibitor. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4880-4. [Content Brief]
[2]. 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 Mar;65(4):707-17. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8974 mL | 9.4869 mL | 18.9739 mL | 47.4347 mL |
| 5 mM | 0.3795 mL | 1.8974 mL | 3.7948 mL | 9.4869 mL | |
| 10 mM | 0.1897 mL | 0.9487 mL | 1.8974 mL | 4.7435 mL | |
| 15 mM | 0.1265 mL | 0.6325 mL | 1.2649 mL | 3.1623 mL | |
| 20 mM | 0.0949 mL | 0.4743 mL | 0.9487 mL | 2.3717 mL | |
| 25 mM | 0.0759 mL | 0.3795 mL | 0.7590 mL | 1.8974 mL | |
| 30 mM | 0.0632 mL | 0.3162 mL | 0.6325 mL | 1.5812 mL | |
| 40 mM | 0.0474 mL | 0.2372 mL | 0.4743 mL | 1.1859 mL | |
| 50 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL | 0.9487 mL | |
| 60 mM | 0.0316 mL | 0.1581 mL | 0.3162 mL | 0.7906 mL | |
| 80 mM | 0.0237 mL | 0.1186 mL | 0.2372 mL | 0.5929 mL | |
| 100 mM | 0.0190 mL | 0.0949 mL | 0.1897 mL | 0.4743 mL |
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