CCT241161 |
رقم الكتالوجGC40054 |
CCT241161 هو مثبط عموم RAF نشط عن طريق الفم مع IC50s من 3 و 6 و 10 و 15 و 30 نانومتر لـ LCK و CRAF و SRC و V600E-BRAF و BRAF ، على التوالييظهر CCT241161 نشاطًا جيدًا في الأورام الميلانينية الطافرة BRAF و NRASيعرض CCT241161 أيضًا نشاط تكاثر الخلايا المضادة للسرطان
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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 .
Average Rating: 5
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