CCT241161 |
| カタログ番号GC40054 |
CCT241161 は、LCK、CRAF、SRC、V600E-BRAF、BRAF の IC50 がそれぞれ 3、6、10、15、30 nM の経口活性汎 RAF 阻害剤です。 CCT241161 は、BRAF および NRAS 変異メラノーマに対して良好な活性を示します。 CCT241161 は、抗がん細胞増殖活性も示します。
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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