SGI-7079
规格
| Cas Number | 1239875-86-5 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 91 mg/mL (199.76 mM); Water: Insoluble; Ethanol: Insoluble; |
| 简短描述 | Axl 抑制剂 |
| 英文简短描述 | Axl Inhibitors |
| 过滤标签 | TAM Receptor,Protein Tyrosine Kinase/RTK |
| 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 | SGI-7079 是一种新型选择性 Axl 抑制剂，体外 IC50 值为 58 nM，能以剂量依赖性方式抑制肿瘤生长，是克服表皮生长因子受体抑制剂耐药性的潜在治疗靶点。 |
| 英文描述 |
Information SGI-7079 SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance. Targets Met ; Mer ; YES ; RET ; FLT3 16051,; In vitro SGI-7079 exhibits a Ki = 5.7 nM for AXL and inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells (EC50 = 100 nM). It inhibits TAM family members MER and Tyro3 similarly as AXL, and shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells express increased levels of the receptor tyrosine kinase Axl and show a trend toward greater sensitivity to the Axl inhibitor SGI-7079. In vivo SGI-7079 inhibits tumor growth in a dose-dependent manner, and at the maximum dose, inhibits tumor growth by 67%, compared with control. the combination of SGI-7079 with erlotinib reverses erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC. Cell Research(from reference) Cell lines：HEK-293 cells Concentrations：0.03, 0.1, 0.3, 1, 3 μmol/L Incubation Time：10 min |