BGB-283 is an orally available dual RAF kinase/EGFR inhibitor. It potently inhibits BRAF family proteins (wild-type ARAF, BRAF, CRAF and BRAF V600E), BRAF(V600E)-activated ERK phosphorylation and cell proliferation, and demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRAF(V600E) and EGFR mutation/amplification. Further, it uniquely displays inhibitory activity towards both BRAF monomeric and dimeric forms, and is considered to be the next generation inhibitor to potentially address resistances associated with increased BRAF dimer formation in response to treatment with first-generation BRAF inhibitors.

KEYWORDS: BGB-283 | Supplier | RAF kinase and EGFR inhibitor | Lifirafenib | BGB283 | BGB 283 | CT-BGB283 | CAS [1446090-77-2] | MEK | RAF | Inhibitor | Enzymes