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Cell Cycle/Checkpoint Aurora Kinase SNS-314 Mesylate

SNS-314 Mesylate

Catalog No. T2617   CAS 1146618-41-8
Synonyms: SNS-314

SNS-314 Mesylate is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). It is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2.

SNS-314 Mesylate, CAS 1146618-41-8
Pack Size Availability Price/USD Quantity
2 mg Inquiry 52.00
5 mg In stock 94.00
10 mg In stock 169.00
25 mg In stock 300.00
50 mg In stock 380.00
100 mg In stock 690.00
1 mL * 10 mM (in DMSO) Inquiry 115.00
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Purity 99.92%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description SNS-314 Mesylate is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). It is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2.
Targets&IC50 Aurora A :ic50 9nM,   Aurora B :ic50 31nM,   Aurora C :ic50 3nM,  
Kinase Assay Aurora-A Kinase Assay: Humanized mouse Aurora A (amino acids 107-403) is expressed in E. coli as described previously. For IC50 assays, compounds are titrated three-fold in DMSO and diluted 12.5-fold into assay buffer (10 mM Tris HCl pH 7.2, 10 mM MgCl2, 0.05% NaN3, 0.01% Tween-20, and 0.1% BSA). Compounds are then diluted 4-fold into assay buffer containing Aurora A and FAM-PKAtide at final concentrations of 2 nM and 50 nM, respectively. The kinase reaction is initiated by adding ATP in assay buffer at a final concentration of 10 mM and incubated at 21 °C for 25 minutes. As a positive control, DMSO is added instead of compound and as a negative control assay buffer is added instead of Aurora A. Both control reactions are conducted in triplicate. To detect phosphorylated PKAtide, the kinase reaction is combined with Progressive Binding Solution (1:400 Progressive Binding Reagent, 1 × Buffer A, Molecular Devices) in a 1:3 ratio. The mixture is incubated for 30 minutes at 21 °C and the plate is scanned on an Analyst AD with excitation at 485 nm and emission at 530 nm. The percent relative enzymatic activity is calculated by normalizing the mP value for each well to the average positive control. Relative enzymatic activity values are plotted as a function of the logarithm of compound concentration and IC50 values are generated in GraphPad Prism software using a sigmoidal dose-response curve-fit. IC50's are calculated as the concentration of compound at which enzymatic activity i
Cell Research
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.(Only for Reference)
Cell lines: HCT116 SCR and HCT116 p53 RNAi cells
Animal Research
Animal Model: HCT116 cells are injected s.c. into the right flank of nu/nu mice.
Synonyms SNS-314
Purity 99.92%
Molecular Weight 527.04
Formula C18H15ClN6OS2·CH4O3S
CAS No. 1146618-41-8

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 52.7 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

15% Captisol: 30 mg/mL

Citations

References and Literature
1. Oslob JD, et al. Bioorg Med Chem Lett, 2008, 18(17), 4880-4884. 2. VanderPorten EC, et al. Mol Cancer Ther, 2009, 8(4), 930-939. 3. Arbitrario JP, et al. Cancer Chemother Pharmacol, 2010, 65(4), 707-717.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Autophagy Compound Library Epigenetics Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Cell cycle related Compound Library

Related Products

Related compounds with same targets
SP-146 Aurora Kinase Inhibitor III SNS-314 Mesylate Aurora inhibitor 1 SCH-1473759 AZD1152 MBM-17S MBM-17

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