BGB283
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 |
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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