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Purity: ≥98%
SNS-314 mesylate, the mesylate salt of SNS314, is a pan-Aurora kinase inhibitor with potential antineoplastic activity. It inhibits Aurora A/B/C with IC50s of 9 nM, 31 nM, and 3 nM, respectively. SNS 314 exhibits excellent antiproliferative activity and high in vivo antitumor efficacy.
| ln Vitro |
SNS-314 inhibits the growth of a wide range of tumor cell lines, including HeLa, PC-3, A2780, MDA-MB-231, H-1299, and HT29. The IC50 values of these cell lines range from 1.8 nM in ovarian cancer cells to 24 nM in colon cancer cells, A2780, and HT29[2].
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| ln Vivo |
The treatment of 50 and 100 mg/kg SNS-314 causes dose-dependent suppression of histone H3 phosphorylation in the HCT116 human colon cancer xenograft model, which lasts for at least 10 hours. SNS-314 exhibits dose-dependent substantial tumor growth inhibition when administered according to a range of regimens, such as weekly, biweekly, or five days on and nine days off[2].
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| 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.
[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 |
| Molecular Formula |
C18H15CLN6OS2.CH4O3S
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|---|---|
| Molecular Weight |
527.04
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| CAS # |
1146618-41-8
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| Related CAS # |
SNS-314;1057249-41-8
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| SMILES |
O=C(NC1=NC=C(CCNC2=C3C(C=CS3)=NC=N2)S1)NC4=CC=CC(Cl)=C4.OS(=O)(C)=O
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| InChi Key |
FYCODPVDEFFWSR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15ClN6OS2.CH4O3S/c19-11-2-1-3-12(8-11)24-17(26)25-18-21-9-13(28-18)4-6-20-16-15-14(5-7-27-15)22-10-23-16;1-5(2,3)4/h1-3,5,7-10H,4,6H2,(H,20,22,23)(H2,21,24,25,26);1H3,(H,2,3,4)
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| Chemical Name |
N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea mesylate
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| Synonyms |
SNS314; SNS 314; SNS-314; SNS-314 mesylate
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 15 mg/mL (28.46 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 150.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: in 15% Captisol: ~6mg/mL (add these co-solvents sequentially from left to right, and one by one), Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1897 mL | 0.9487 mL | 1.8974 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
CI50screening process of SNS-314 with cytotoxic anticancer agents.Mol Cancer Ther.2009 Apr;8(4):930-9. |
SNS-314 combined with spindle toxins vincristine (VIN) or docetaxel (DTX) compromises the spindle checkpoint.Mol Cancer Ther.2009 Apr;8(4):930-9. |
Effects of SNS-314 combinations with docetaxel (DTX) or vincristine (VIN) under a sequential administration schedule.Mol Cancer Ther.2009 Apr;8(4):930-9. |
Combination of SNS-314 with spindle toxins results in synergistic inhibition of cell growth.Mol Cancer Ther.2009 Apr;8(4):930-9. |
Sequential SNS-314/docetaxel dosing results in significant antitumor activity.Mol Cancer Ther.2009 Apr;8(4):930-9. |
SNS-314 demonstrates significant and prolonged anti-tumor activity using flexible dosing schedules in HCT116 colon cancer xenografts.Cancer Chemother Pharmacol.2010 Mar;65(4):707-17. |
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