CCT241161 |
| Catalog No.GC40054 |
CCT241161은 LCK, CRAF, SRC, V600E-BRAF 및 BRAF에 대해 IC50이 각각 3, 6, 10, 15 및 30nM인 경구 활성 범RAF 억제제입니다. CCT241161은 BRAF 및 NRAS 돌연변이 흑색종에서 우수한 활성을 나타냅니다. CCT241161은 또한 항암 세포 증식 활성을 나타냅니다.
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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