BGB283

  • Chemical Properties
CAS No. 1446090-77-2 Cat. No. BCP09509
Name BGB283
Synonyms BGB-283;BGB 2833; Beigene-283; Beigene283; Beigene 283; Lifirafenib;
Formula C25H17F3N4O3 M. Wt 478.42
  • Biological Activity
Description BGB-283, also known as Beigene-283 or Lifirafenib, is a Novel potent and selective RAF Kinase and EGFR inhibitor. BGB-283-displays Potent Antitumor Activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 potently inhibits B-RAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harbouring B-RAFV600E and EGFR mutation/amplification. In B-RAFV600E CRC cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. In vivo, BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell-line derived and primary human colorectal tumor xenografts bearing B-RAFV600E mutation. BGB-283 as a potent antitumor drug candidate with clinical potential for treating CRC harbouring B-RAFV600E mutation.
Pathways Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway MAPK Pathway 
Targets EGFR Raf 

Structure

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