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CCT196969 is a small molecule dual inhibitor of the SRC family kinases (SFK) and RAF kinases (including BRAF and CRAF). Developed by the Institute of Cancer Research (ICR), it is designed to overcome resistance to standard BRAF inhibitors in melanoma by simultaneously targeting the MAPK pathway and the compensatory SRC signaling pathway. Preclinical studies have demonstrated its efficacy in inhibiting proliferation, migration, and survival of melanoma cells, including those that have metastasized to the brain and those resistant to conventional BRAF inhibitors. It acts by reducing the phosphorylation of downstream signaling molecules such as ERK, MEK, and STAT3.
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