CEP-32496 | CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf, the Kd was 14 nM/36 nM and 39 nM, moderately effective at Abl-1, c-Kit, Ret, PDGFR and VEGFR2, with weak affinity for MEK-1, MEK-2, ERK-1 and ERK-2. at present, BRAF inhibitors can be divided into two categories, one is multi-target kinase inhibitors, including BRAF, including a variety of kinase inhibition, such as Sorafenib (Sorafenib), regorafenib, Pazopanib, ASN-003(Asana) and CEP-32496 (Ambit biological Ambit and Teva), etc. This kind of inhibitor has a broad spectrum of anti-tumor and anti-angiogenesis effect, the indication is wide, as the first BRAF inhibitor Sorafenib, is the first line of advanced liver cancer, kidney cancer treatment drugs, annual sales were all above $1.1 billion between 2012 and 2016. Another class of BRAF V600E inhibitors have high inhibitory activity on BRAF, especially BRAF V600E. These inhibitors are mainly used in the treatment of melanoma, such as Vemurafenib, Dabrafenib, PLX-8394 and Encorafenib, etc. |