SNS-314

SNS-314 is a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.

Product information

CAS Number: 1057249-41-8

Molecular Weight: 430.93

Formula: C18H15ClN6OS2

Synonym:

SNS314

SNS 314

SNS-314 free base

Related CAS Number:

1146618-41-8 (SNS-314 mesylate)

Chemical Name: N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3, 2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea.

Smiles: O=C(NC1=NC=C(CCNC2=NC=NC3C=CSC=32)S1)NC1=CC(Cl)=CC=C1

InChiKey: FAYAUAZLLLJJGH-UHFFFAOYSA-N

InChi: InChI=1S/C18H15ClN6OS2/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/h1-3,5,7-10H,4,6H2,(H,20,22,23)(H2,21,24,25,26)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 105 mg/mL(243.65 mM). Water: 6 mg/mL(13.92 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. A recent study shows that SNS-314 Mesylate shows potent antiproliferative activity in HCT116 cells and inhibits soft agar colony formation.

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. 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.

References:

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

Products are for research use only. Not for human use.