CCT196969 is a paradox-breaking pan RAF Inhibitor, targeting simultaneously RAF and SFKs. BRAF and MEK inhibitors are effective in treating BRAF mutant melanoma however most patients eventually relapse with acquired resistance, and others present intrinsic resistance to these drugs. Resistance is often mediated by pathway reactivation through receptor tyrosine kinase (RTK)/SRC-family kinase (SFK) signaling or mutant NRAS, which drive paradoxical reactivation of the pathway. By targeting pan RAF and SFKs, CCT196969 demonstrates efficacious inhibitory activity towards MEK/ERK in BRAF and NRAS mutant melanoma, while showing no effect on paradoxical pathway activation.

KEYWORDS: CCT196969 | Supplier | pan-Raf inhibitor | CCT-196969 | CCT 196969 | CT-CCT196 | CAS [1163719-56-9] | MEK | RAF | Inhibitor | Enzymes