CCT241161

CCT241161 is an orally active pan-RAF inhibitor with IC₅₀s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity^[1]. IC50 & Target: IC50: 3 nM (LCK), 10 nM (SRC)^[1]. In Vitro: CCT241161 (1, 3, 10, 30, 100 nM; 24 h) inhibits MEK and ERK in WM266.4 cells^[1].
CCT241161 (1, 10, 100 nM and 1, 10, 100 µM) inhibits BRAF^V600E in Ba/F3 cells^[1].
CCT241161 (0.5 µM; 20 days) inhibits A375 cell but not cause drug resistance^[1].
CCT241161 (1 µM , 4 h) inhibits BRAF-inhibitor-resistant melanoma cells^[1].
CCT241161 (0.1, 0.3, 1, 3, 10 µM; 24 h) inhibits MEK in NRAS mutant cells^[1].
CCT241161 (0.1, 1, 10, 100 µM) shows anti-proliferative activity in D04 cells^[1]. In Vivo: CCT241161 (10, 20 mg/kg; i.g; once a day for 7 days) inhibits the growth of BRAF mutant A375, PLX4720-resistant A375 and NRAS mutant DO4 tumor xenografts in mice^[1].