BRAF Kinase

Many tumors exhibit a high frequency of mutation in the BRAF kinase. Melanoma is the most significant with a 60-70% mutation rate, followed by colon with a 20% mutation rate and glioblastoma with a 12% mutation rate.

Using its KINOMEscan technology, Ambit has identified multiple series of BRAF inhibitors with sub-micromolar potency. Two of these programs are currently undergoing lead optimization, and Ambit intends to advance a BRAF inhibitor into clinical trials in 2008.