PLX7904
规格
| Cas Number | 1393465-84-3 |
| 规格或纯度 | ≥97% |
| 纯度 | ≥97% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (195.11 mM); Water: Insoluble; Ethanol: Insoluble; |
| 简短描述 | Raf抑制剂 |
| 英文简短描述 | Raf Inhibitors |
| 过滤标签 | Raf,MAPK/ERK Pathway |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | PLX7904又名PB04，是一种强效、选择性的RAF断裂抑制剂。它能有效抑制突变 BRAF 黑色素瘤细胞中 ERK1/2 的激活，但不会过度激活突变 RAS 表达细胞中的 ERK1/2。 |
| 英文描述 |
Information PLX7904 PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Targets Raf In vitro PLX7940 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.Consistent with ERK1/2 re-activation driving the re-acquisition of malignant properties, PLX7904 promotes apoptosis and inhibits entry into S phase and anchorage-independent growth in mutant N-RAS mediated vemurafenib-resistant cells.PLX7904 is also evaluated in the human SCC cell line A431 and the human breast adenocarcinoma cell line SKBR3 as these cells achieve MAPK pathway activation by upstream signals feeding into RAS (through overexpression of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), respectively). In vivo PLX7904 inhibits the COLO205 xenograft growth in eight mice per group. Cell Research(from reference) Cell lines：WM793, WM115, WM9, WM278, WM1346, WM1366, WM1361A, Sbcl2, 1205Lu, A375, SK-MEL 24, SKMEL-2, and SK-MEL 207 cells Concentrations：0, 0.5, 1, 5 μM Incubation Time：24 h |