store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 44.00 | |
5 mg | In stock | $ 105.00 | |
10 mg | In stock | $ 172.00 | |
25 mg | In stock | $ 333.00 | |
50 mg | In stock | $ 589.00 | |
100 mg | In stock | $ 919.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 153.00 |
Description | Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively. |
Targets&IC50 | B-Raf (V600E):23 nM, EGFR:29 nM, EGFR (L858R/T790M ):495 nM (IC50) |
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.BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation,in BRAFV600E colorectal cancer cell lines. It demonstrates selective cytotoxicity to cell lines harboring BRAFV600E or EGFR mutations. In A431 cells, BGB-283 inhibits the EGF-induced EGFR autophosphorylation on Tyr1068 in a dose-dependent manner. In WiDr colorectal cancer cells, BGB-283 inhibits the feedback activation of EGFR signaling and achieves sustained inhibition of pERK[1] |
In vivo | The treatment of BGB-283 leads to tumor growth inhibition accompanied by partial and complete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearing BRAFV600E mutation in a dose-dependent manner. BGB-283 has high efficacy in BRAF(V600E) colorectal cancer xenograft models, including Colo205, HT29, 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 EGFR and ERK1/2 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 DUSP6 expression, ERK and MEK phosphorylation in vivo when dosed repeatedly. There is no detectable difference on AKT phosphorylation[1]. |
Synonyms | BGB-283, Beigene-283 |
Molecular Weight | 478.42 |
Formula | C25H17F3N4O3 |
CAS No. | 1446090-79-4 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (209.02 mM)
You can also refer to dose conversion for different animals. More
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Lifirafenib 1446090-79-4 Angiogenesis JAK/STAT signaling MAPK Tyrosine Kinase/Adaptors Raf EGFR Epidermal growth factor receptor ErbB-1 inhibit BGB-283 Raf kinases Beigene-283 Inhibitor HER1 BGB 283 BGB283 inhibitor