-
Catalog Number:
E1KS1145 Amount:
5mg1 PHYSICAL AND CHEMICAL PROPERTIES Storage/Stability:
at -20℃ 2 years
2 Biological Activity
SNS-032 (BMS-387032) is a potent and selective cyclin-dependent kinases (CDK) 9, 7 and 2 inhibitor with IC50 of 4, 62 and 38 nM for CDK9, CDK2/cyclin A and CDK7/Cyclin H, respectively. SNS-032(BMS-387032) is used in the treatment of B-cell malignancies and advanced solid tumors. Preclinical studies have shown that SNS-032 is a specific and potent inhibitor of CDK2, 7 and 9 which induces cell cycle arrest and apoptosis in tumor cell lines. SNS-032(BMS-387032) was shown to inhibit in vitro angiogenesis and prostaglandin E2 (PGE2) production, both strongly associated with tumorigenesis. Phase I clinical trials support the safety and tolerability of SNS-032 as evaluated in dose-escalation studies. SNS-032(BMS-387032) is currently administered by i.v. infusion but has shown promising potential for oral delivery. [1] [2][3]
3 References:
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 Hai-yun Xiao, Kyoung S. Kim,et al. J. Med. Chem 2004;47:1719-1728
SNS-032 Prevents Tumor Cell–Induced Angiogenesis By Inhibiting Vascular Endothelial Growth Factor1 M. Aktar Ali,Hak Choy,et al. Neoplasia May 2007;9:370 – 381
A phase 1 study of SNS-032 (formerly BMS-387032),a potent inhibitor of cyclin-dependent kinases 2, 7 and 9 administered as a single oral dose and weekly infusion in patients with metastatic refractory solid tumors Elisabeth I. Heath,Keith Bible,et al. Invest New Drugs 2008;26:59–65
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.