For research use only. Not for therapeutic Use.
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.
| Catalog Number | I006580 |
| CAS Number | 1581764-31-9 |
| Synonyms | EBI-907; EBI 907; EBI907; CAS# 1581764-31-9;N-(2-chloro-3-(1-cyclopropyl-8-methoxy-3H-pyrazolo[3,4-c]isoquinolin-7-yl)-4-fluorophenyl)-3-fluoropropane-1-sulfonamide |
| Molecular Formula | C23H21ClF2N4O3S |
| Purity | ≥95% |
| Target | B-RafV600E inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4°C for short term or -20 °C for long term |
| Reference | </br>1:EBI-907, a novel BRAF(V600E) inhibitor, has potent oral anti-tumor activity and a broad kinase selectivity profile. Zhang J, Lu B, Liu D, Shen R, Yan Y, Yang L, Zhang M, Zhang L, Cao G, Cao H, Fu B, Gong A, Sun Q, Wan H, Zhang L, Tao W, Cao J.Cancer Biol Ther. 2016;17(2):199-207. doi: 10.1080/15384047.2016.1139231. Epub 2016 Jan 25. PMID: 26810733 Free PMC Article</br>2:Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers. Lu B, Cao H, Cao J, Huang S, Hu Q, Liu D, Shen R, Shen X, Tao W, Wan H, Wang D, Yan Y, Yang L, Zhang J, Zhang L, Zhang L, Zhang M.Bioorg Med Chem Lett. 2016 Feb 1;26(3):819-23. doi: 10.1016/j.bmcl.2015.12.086. Epub 2015 Dec 24. PMID: 26739779 |
