2. Academic Validation
  3. 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

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

  • J Med Chem. 2011 Oct 27;54(20):7066-83. doi: 10.1021/jm2006222.
Vito Guagnano 1,  Pascal Furet,  Carsten Spanka,  Vincent Bordas,  Mickaël Le Douget,  Christelle Stamm,  Josef Brueggen,  Michael R Jensen,  Christian Schnell,  Herbert Schmid,  Markus Wartmann,  Joerg Berghausen,  Peter Drueckes,  Alfred Zimmerlin,  Dirksen Bussiere,  Jeremy Murray,  Diana Graus Porta
Affiliations

Affiliation

  • 1 Novartis Institute for BioMedical Research, CH-4002 Basel, Switzerland. vito.guagnano@novartis.com
PMID: 21936542 DOI: 10.1021/jm2006222
Abstract

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.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z