Product Name: BGJ-398

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CAT#: A-1143


  Synonym:NVP-BGJ398, BGJ398, BG-J398

BGJ-398 Chemical Structure BGJ-398 chemical structure


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IUPAC/Chemical name: 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea.

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Biological Activity

BGJ398 is a pan FGFR kinase inhibitor, and is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. pan FGFR kinase inhibitor BGJ398 selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs are a family of receptor tyrosine kinases which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival.

Technical Data
Formula:     C26H31Cl2N7O3
M.Wt:      560.49
CAS#: 872511-34-7
Solubility : Chloroform, DMSO, Methanol
Purity: >99%
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 2 years.
BGJ-398 MSDS BGJ-398 CoA

Reference
Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
http://pubs.acs.org/doi/abs/10.1021/jm2006222
A novel series of N-aryl-N-pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the fibroblast growth factor receptor tyrosine kinases 1, 2, and 3 by rationally designing the substitution pattern of the aryl ring. On the basis of its in vitro profile, compound 1h (NVP-BGJ398) was selected for in vivo evaluation and showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3. These results support the potential therapeutic use of 1h as a new anticancer agent.

The DDR is in
J Kotz - SciBX: Science-Business eXchange, 2011 - nature.com
...samples had genomic amplification of the tyrosine kinase fibroblast growth factor receptor 1 (FGFR1; CD331).2,3 Thomas told SciBX that based on those results his team is now enrolling patients with FGFR1-amplified lung SCC in a Phase I trial of Novartis AG's BGJ398, a pan...


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