CCT241161 是一种具有口服活性的泛 RAF 抑制剂，对 LCK、CRAF、SRC、V600E-BRAF 和 BRAF 的 IC50 分别为 3、6、10、15 和 30 nM。 CCT241161 在 BRAF 和 NRAS 突变黑色素瘤中显示出良好的活性。 CCT241161 还表现出抗癌细胞增殖活性。
| Cas No. | 1163719-91-2 |
| Canonical SMILES | O=C1NC2=NC=CC(OC3=CC=C(NC(NC4=CC(C(C)(C)C)=NN4C5=CC=CC=C5)=O)C(SC)=C3)=C2N=C1 |
| 分子式 | C28H27N7O3S |
| 分子量 | 541.6 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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