CCT241161 |
| Catalog No.GC40054 |
CCT241161 est un inhibiteur pan-RAF actif par voie orale avec des IC50 de 3, 6, 10, 15 et 30 nM pour LCK, CRAF, SRC, V600E-BRAF et BRAF, respectivement. CCT241161 montre une bonne activité dans les mélanomes mutants BRAF et NRAS. CCT241161 présente également une activité proliférative des cellules anticancéreuses.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1163719-91-2
Sample solution is provided at 25 µL, 10mM.
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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 .
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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