For research use only. Not for therapeutic Use.
Lifirafenib(Cat No.:I014444), also referred to as BGB-283 or Beigene-283, is a potent inhibitor of RAF family kinases and EGFR (Epidermal Growth Factor Receptor) activities. In biochemical assays, it demonstrates IC50 values of 23, 29, and 495 nM for the recombinant BRAFV600E kinase domain, EGFR, and EGFR T790M/L858R mutant, respectively. By inhibiting these kinases and the EGFR pathway, Lifirafenib holds potential as a targeted therapy for cancers driven by aberrant activation of these signaling pathways, particularly those associated with BRAF mutations and EGFR mutations such as T790M/L858R.
Catalog Number | I014444 |
CAS Number | 1446090-79-4 |
Synonyms | Lifirafenib; BGB-283; Beigene-283;5-(((1R,1aS,6bR)-1-(6-(Trifluoromethyl)-1H-benzimidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa(b)benzofuran-5-yl)oxy)-3,4-dihydro-1H-1,8-naphthyridin-2-one |
Molecular Formula | C25H17F3N4O3 |
Purity | ≥95% |
Target | EGFR; Raf |
Solubility | Soluble in DMSO |
IUPAC Name | 5-[[(1R,1aS,6bR)-1-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-5-yl]oxy]-3,4-dihydro-1H-1,8-naphthyridin-2-one |
InChI | InChI=1S/C25H17F3N4O3/c26-25(27,28)11-1-4-15-16(9-11)31-24(30-15)21-20-14-10-12(2-5-17(14)35-22(20)21)34-18-7-8-29-23-13(18)3-6-19(33)32-23/h1-2,4-5,7-10,20-22H,3,6H2,(H,30,31)(H,29,32,33)/t20-,21-,22-/m0/s1 |
InChIKey | NGFFVZQXSRKHBM-FKBYEOEOSA-N |
SMILES | C1CC(=O)NC2=NC=CC(=C21)OC3=CC4=C(C=C3)OC5C4C5C6=NC7=C(N6)C=C(C=C7)C(F)(F)F |
Reference | </br>[1] Tang Z, et al. Mol Cancer Ther. 2015, 14(10):2187-97. </br> |