SNS 032

Biological Activity

SNS 032 is a cyclin dependent kinase (cdk) inhibitor (reported IC₅₀ values are 0.004 - 0.048, 0.0045 - 0.05, 0.062 - 0.29, 0.2-0.48, 0.4 and 0.45 μM for cdk9, cdk2, cdk7, cdk1, cdk5 and cdk4, respectively). Displays no activity against 190 additional kinases (IC₅₀ >1 μM). Arrests the cell cycle at G₂/M; inhibits transcription, proliferation and colony formation, and induces apoptosis in RPMI-8226 multiple myeloma cells. Prevents tumor cell-induced VEGF secretion and in vitro angiogenesis.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
   Jorda et al.
   J.Med.Chem., 2018;61:9105
2. SNS-032 prevents tumor cell-induced angiogenesis by inhibiting vascular endothelial growth factor.
   Ali et al.
   Neoplasia, 2007;9:370
3. SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples.
   Conroy et al.
   Cancer Chemother.Pharmacol., 2009;64:723
4. Responses in mantle cell lymphoma cells to SNS-032 depend on the biological context of each cell line.
   Chen et al.
   Cancer Res., 2010;70:6587
5. N-(Cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent
   Misra et al.
   J.Med.Chem., 2004;47:1719

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