Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf and EGFR, respectively.
IC50&Target
EGFR
29 nM (IC50)
BRaf
23 nM (IC50)
EGFR
495 nM (IC50)
体外研究
Lifirafenib (BGB-283) potently inhibits BRaf-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRaf and EGFR mutation/amplification. In BRaf colorectal cancer cell lines, Lifirafenib (BGB-283) effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation.
体内研究
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 BRaf mutation.
分子式
C25H17F3N4O3
分子量
478.42
CAS号
1446090-79-4
运输条件
Room temperature in continental US; may vary elsewhere.