Lifirafenib(BGB-283)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29nM。
货号:ajcx30922
CAS:1446090-79-4
分子式:C25H17F3N4O3
分子量：478.42
溶解度:DMSO: ≥ 100 mg/mL (209.02 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.

Lifirafenib (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, Lifirafenib (BGB-283) effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation[1].

Lifirafenib (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[1].

[1]. Tang Z, et al. BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.