Home MAPK Raf inhibitor - EGFR inhibitor Lifirafenib (BGB-283) For research use only.

Lifirafenib (BGB-283)

Synonyms: Beigene-283

Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.

Lifirafenib (BGB-283) Chemical Structure

Lifirafenib (BGB-283) Chemical Structure

CAS: 1446090-79-4

Selleck's Lifirafenib (BGB-283) has been cited by 6 publications

Purity & Quality Control

Batch: S792601 DMSO] 95 mg/mL] false] Ethanol] 95 mg/mL] false] Water] Insoluble] false Purity: 99.73%
99.73

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Biological Activity

Description Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.
Targets
WT A-RAF [1]
(Cell-free assay)		 C-RAF (Y340/341D) [1]
(Cell-free assay)		 BRAF(V600E) [1]
(Cell-free assay)		 EGFR [1]
(Cell-free assay)		 BRAF WT [1]
(Cell-free assay)		 Click to View More Targets
1 nM 7 nM 23 nM 29 nM 32 nM
In vitro
In vitro In vitro, BGB-283 potently inhibits BRAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRAFV600E and EGFR mutation/amplification. In BRAFV600E colorectal cancer cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. It demonstrates selective cytotoxicity to cell lines harboring BRAFV600E or EGFR mutations. BGB-283 inhibits the EGF-induced EGFR autophosphorylation on Tyr1068 in A431 cells in a dose-dependent manner. In WiDr colorectal cancer cells, BGB-283 is shown to be able to inhibit the feedback activation of EGFR signaling and achieves sustained inhibition of pERK[1].
Cell Research Cell lines A375 cells
Concentrations 0.03, 1, 10 μM
Incubation Time 3 days
Method

The number of cells seeded per well of a 96-well plate is optimized for each cell line to ensure logarithmic growth over the 3 days treatment period. Cells are left to attach for 16 hours and then treated with a 10-point dilution series in duplicate. Following a 3-day exposure to the compound, a volume of CellTiter-Glo reagent equal to the volume of cell culture medium present in each well is added. Mixture is mixed on an orbital shaker for 2 minutes to allow cell lysing, followed by 10 minutes incubation at room temperature to allow development and stabilization of luminescent signal. Luminescent signal is measured
In Vivo
In vivo 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 BRAFV600E mutation. BGB-283 is highly efficacious in BRAF(V600E) colorectal cancer xenograft models, including HT29, Colo205, and two primary tumor xenografts harboring BRAFV600E mutation. In addition, BGB-283 shows compelling efficacy in a WiDr xenograft model where EGFR reactivation is shown to be induced upon BRAF inhibition. BGB-283 induces tumor regression in HCC827 but not in A431 xenograft. BGB-283 inhibits phosphorylation of both ERK1/2 and EGFR and displays potent antitumor activity in WiDr tumor xenografts. BGB-283 does not induce EGFR feedback activation as reported for vemurafenib. BGB-283 potently inhibits MEK and ERK phosphorylation and DUSP6 expression in vivo when dosed repeatedly. There is no detectable difference on AKT phosphorylation[1].
Animal Research Animal Models NOD/SCID and BALB/c nude mice
Dosages 2.5 to 30 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 478.42 Formula

C25H17F3N4O3
CAS No. 1446090-79-4 SDF Download Lifirafenib (BGB-283) SDF
Smiles C1CC(=O)NC2=NC=CC(=C21)OC3=CC4=C(C=C3)OC5C4C5C6=NC7=C(N6)C=C(C=C7)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 95 mg/mL ( (198.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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