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Lifirafenib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lifirafenib图片
CAS NO:1446090-79-4
包装与价格:
包装价格(元)
5 mg电议
100 mg电议
500 mg电议

产品名称
BGB-283
Beigene-283
产品介绍
LifiRafenib 是新型高效的Raf激酶和EGFR抑制剂,对重组BRafV600E和EGFR的IC50值分别为 23 和 29 nM。

产品描述

Lifirafenib 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.

体外活性

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]

体内活性

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].

Cas No.

1446090-79-4

分子式

C25H17F3N4O3

分子量

478.42

别名

BGB-283;Beigene-283

储存和溶解度

DMSO:100 mg/mL (209.02 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years