Lifirafenib (Synonyms: BGB-283) |
| رقم الكتالوجGC60992 |
Lifirafenib (BGB-283) هو مثبط جديد وقوي لـ Raf Kinase و EGFR بقيم IC50 تبلغ 23 و 29 نانومتر من أجل BRafV600E و EGFR المؤتلف ، على التوالي
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Cas No.: 1446090-79-4
Sample solution is provided at 25 µL, 10mM.
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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.
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