| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408286-1ml |
1ml |
现货  |
|
| 别名 | 替拉替尼 |
|---|---|
| 英文别名 | BAY 57-9352 | 4-((4-(4-chlorophenylamino)furo[2,3-d]pyridazin-7-yloxy)methyl)-N-methylpicolinamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Telatinib |
| 生化机理 | 替拉替尼（BAY 57-9352）是血管内皮生长因子受体2/3、c-Kit和表皮生长因子受体α的强效抑制剂，IC50分别为6 nM/4 nM、1 nM和15 nM。第二阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 血管内皮生长因子受体 3 抑制剂 |
| 产品介绍 |
Information Telatinib (BAY 57-9352) is a potent inhibitor ofVEGFR2/3,c-Kitand PDGFRα withIC50of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2. Telatinib has 0.66, 0.17, and 2.5 times higher IC50 values for VEGFR3, c-Kit, and PDGFRβ than VEGFR2, respectively, while Vatalanib exhibits 18, 20, and 16 times higher IC50 values, respectively, indicating that Telatinib has potential benefit over Vatalanib. Telatinib inhibits VEGFR2 autophosphorylation in a whole-cell assay with an IC50 of 19 nM, suppresses VEGF-dependent proliferation of human umbilical vein endothelial cells with an IC50 of 26 nM, and blocks PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM. Telatinib displays little inhibitory activity against the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, and the Tie-2 receptor. In vivo Given that tumor development and metastasis are ascribed to deregulated VEGFR signal pathway, Telatinib treatment significantly inhibits tumor growth and metastasis by blocking the VEGFR signaling and subsequently tumor angiogenesis. In addition to the significant inhibition of tumor angiogenesis, Telatinib treatment induces a significant decrease in endothelium-dependent and endothelium-independent vasodilation, as well as reduction in capillary density, leading to an increase in systolic and diastolic blood pressure. Administration of Telatinib as a single agent exhibits a potent anti-tumor activity in multiple human tumor xenograft models including MDA-MB-231 breast cancer, Colo-205 colon cancer, DLD-1 colon cancer, and H460 non-small cell lung cancer, as well as pancreatic and prostate carcinoma in a dose-dependent manner. cell lines：U87MG, A549 and H838 cells Concentrations： Incubation Time： Powder Purity:≥97% |
| IC50 | PDGFRα, IC50: 15 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CNC(=O)C1=NC=CC(=C1)COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4 |
| 分子量 | 409.83 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 6 mg/mL (23.78 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
首页
400-620-6333
