1. Cell Cycle/DNA Damage Epigenetics
  2. Aurora Kinase
  3. SNS-314 mesylate

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.

For research use only. We do not sell to patients.

SNS-314 mesylate Chemical Structure

SNS-314 mesylate Chemical Structure

CAS No. : 1146618-41-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of SNS-314 mesylate:

Top Publications Citing Use of Products

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

Aurora A

9 nM (IC50)

Aurora B

31 nM (IC50)

Aurora C

6 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HCT-116 EC50
< 16 nM
Compound: 21, SNS-314
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
[PMID: 18678489]
HCT-116 EC50
< 16 nM
Compound: 1c
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
[PMID: 19646866]
HCT-116 EC50
< 16 nM
Compound: 21, SNS-314
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
[PMID: 18678489]
HCT-116 EC50
6 nM
Compound: 11, SNS-314
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
[PMID: 19320489]
HCT-116 EC50
6 nM
Compound: 1c
Antiproliferative activity against human HCT116 cells by BrdU incorporation assay
Antiproliferative activity against human HCT116 cells by BrdU incorporation assay
[PMID: 19646866]
In Vitro

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.

In Vivo

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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

527.04

Formula

C19H19ClN6O4S3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=CC=CC(Cl)=C1)NC2=NC=C(S2)CCNC3=C4C(C=CS4)=NC=N3.OS(C)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8974 mL 9.4869 mL 18.9739 mL
5 mM 0.3795 mL 1.8974 mL 3.7948 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 15 mg/mL (28.46 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 15 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (150.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Kinase Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

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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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SNS-314 mesylate
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