| Hazard Information | Back Directory | [Description]
EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases including BRK, FGFR1, c-Kit, and PDGFRb. | [Uses]
EBI-907 is an orally active and highly potent B-RafV600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-RafV600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-RafV600E associated cancers[1][2]. | [References]
[1] Lu B, et al. Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers. Bioorg Med Chem Lett. 2016 Feb 1;26(3):819-823. DOI:10.1016/j.bmcl.2015.12.086
[2] Zhang J, et al. EBI-907, a novel BRAF(V600E) inhibitor, has potent oral anti-tumor activity and a broad kinase selectivity profile. Cancer Biol Ther. 2016;17(2):199-207. DOI:10.1080/15384047.2016.1139231 |
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