| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408268-1ml |
1ml |
现货  |
|
| 英文别名 | N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Axitinib (AG 013736) |
| 生化机理 | 阿西替尼（AG 013736）是一种多靶点抑制剂，可抑制 VEGFR1、VEGFR2、VEGFR3、PDGFRβ 和 c-Kit，在猪主动脉内皮细胞中的 IC50 分别为 0.1 nM、0.2 nM、0.1-0.3 nM、1.6 nM 和 1.7 nM。 |
| 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抑制剂 |
| 产品介绍 |
应用： 阿昔替尼已被用作血管内皮生长因子 (VEGF) 受体酪氨酸激酶抑制剂 (TKI) ，以研究其对肾癌细胞体外增殖的影响。 此外，在调理水 (CW) 中维持的脱氯胚胎中，它还用于抑制肠系膜上动脉 (AMA) 血管生成。 Information Axitinib (AG 013736) is a multi-target inhibitor ofVEGFR1,VEGFR2,VEGFR3, PDGFRβ and c-Kit withIC50of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC). In vivo Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma. cell lines：DLBCL cells, SUDHL-6 cells Concentrations：1 nM - 10 μM Incubation Time：72 hours Powder Purity:≥99% |
| ALogP | 4.2 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)/C=C/C4=CC=CC=N4 |
| 分子量 | 386.47 |
| Reaxy-Rn | 14436737 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14436737&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 50 mg/mL (199.77 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
| WGK Germany | 3 |
|---|
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