BGB-283( Lifirafenib | BGB 283 | BGB283 )

Catalog No. M11891 CAS No. 1446090-77-2

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Product Name

BGB-283
Note

Research use only, not for human use.
Brief Description

BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM).
Description

BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM); inhibits recombinant BRAFV600E with IC50 of 23 nM; also inhibits EGFR and EGFR T790M/L858R with IC50 of 29 nM and 495 nM respectively; potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation in vitro; shows tumor growth inhibition in both cell line-derived and primary human colorectal tumor xenografts bearing BRAF(V600E) mutation.Colon Cancer Preclinical.
In Vitro

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In Vivo

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Synonyms

Lifirafenib | BGB 283 | BGB283
Pathway

MAPK/ERK Signaling
Target

Raf
Recptor

Raf
Research Area

Cancer
Indication

Colon Cancer

CAS Number

1446090-77-2
Formula Weight

478.4227
Molecular Formula

C25H17F3N4O3
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 125 mg/mL
SMILES

[H][C@@]1(C2=CC(OC3=C(CCC4=O)C(N4)=NC=C3)=CC=C2O[C@]51[H])[C@@H]5C6=NC7=CC=C(C=C7N6)C(F)(F)F
Chemical Name

1,8-Naphthyridin-2(1H)-one, 5-[[(1R,1aS,6bR)-1a,6b-dihydro-1-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1H-cyclopropa[b]benzofuran-5-yl]oxy]-3,4-dihydro-, rel-

1. Tang Z, et al. Mol Cancer Ther. 2015 Oct;14(10):2187-97. 2. Cancer Discov. 2016 Jul;6(7):OF1.

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