CCT241161 |
Catalog No.GC40054 |
CCT241161 es un inhibidor pan-RAF activo por vÍa oral con IC50 de 3, 6, 10, 15 y 30 nM para LCK, CRAF, SRC, V600E-BRAF y BRAF, respectivamente. CCT241161 muestra una buena actividad en los melanomas mutantes BRAF y NRAS. CCT241161 también exhibe actividad proliferativa de células anticancerÍgenas.
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Cas No.: 1163719-91-2
Sample solution is provided at 25 µL, 10mM.
CCT241161 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 252, 15, 6, 15, and 3 nM, respectively). It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 µM. CCT241161 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner. In vivo, CCT241161 (20 mg/kg per day) induces tumor regression in a B-RAF mutant A375 mouse xenograft model. CCT241161 also inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant patient-derived xenograft (PDX) mouse models including those resistant to both dabrafenib and trametinib .
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