BGB283
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CAS No. | 1446090-77-2 | Cat. No. | BCP09509 |
Name | BGB283 | ||
Synonyms | BGB-283;BGB 2833; Beigene-283; Beigene283; Beigene 283; Lifirafenib; | ||
SMILES | C1CC(=O)NC2=NC=CC(=C21)OC3=CC4=C(C=C3)OC5C4C5C6=NC7=C(N6)C=C(C=C7)C(F)(F)F | ||
Chemical Name | |||
Formula | C25H17F3N4O3 | M. Wt | 478.42 |
Purity | 98% | Storage | Store at 4-8°C |
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. |
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