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- CAS号：
1035270-39-3
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥226.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥502.0 |
| 规格： | 5mg | 产品价格： | ￥492.0 |
| 规格： | 10mg | 产品价格： | ￥634.0 |
| 规格： | 25mg | 产品价格： | ￥1016.0 |
| 规格： | 50mg | 产品价格： | ￥1536.0 |
| 规格： | 100mg | 产品价格： | ￥2152.0 |
Product Introduction
Bioactivity
| 名称 | AZD4547 |
| 描述 | AZD4547 is an FGFR family inhibitor. AZD4547 selectively inhibits FGFR1 phosphorylation and suppresses cancer cell proliferation through inhibition of FGFR1 signaling, and is able to act on FGFR1 (IC50:0.2 nM), FGFR2 (IC50:2.5 nM), FGFR3 (IC50:1.8 nM) and FGFR4 (IC50:165 nM). IC50:165 nM).[2] |
| 细胞实验 | Cell lines were incubated with fixed concentrations of AZD4547 for 72 hours. For fluorescence-activated cell sorting (FACS), cells were fixed with 70% ethanol and then incubated with propidium iodide/RNase A labeling solution. Cell-cycle profiles were assessed with a FACSCalibur instrument and CellQuest analysis software. For apoptotic analysis, cells and media were gently harvested and centrifuged, followed by washing of cell pellets. Cells were then processed for Annexin V-fluorescein isothiocyanate (FITC) staining and propidium iodide uptake according to the manufacturer's instructions. The proportion of cells staining positive for Annexin V were then assessed with a FACSCalibur instrument and quadrant sorting was done by CellQuest analysis software [1]. |
| 激酶实验 | Cells were treated with AZD4547 or control for 3 hours at 37°C and then stimulated with 10 ng/mL aFGF/bFGF and 10 μg/mL heparin for 20 minutes. Western blotting was conducted with standard SDS-PAGE procedures and antibody incubation carried out overnight at 4°C. Secondary antibodies were applied and immunoreactive proteins visualized with Chemiluminescence substrate according to the manufacturer's instructions [1]. |
| 动物实验 | Tumor xenografts were established by s.c. injection into the left flank with 0.1 mL tumor cells (1 × 10^6 for LoVo, 1 × 10^7 for HCT-15, and 1 × 10^7 for Calu-6) or 0.2 mL (2 × 10^7 for KMS11 and KG1a) mixed 1:1 with Matrigel, with the exception of LoVo and HCT-15, which did not include Matrigel. Mice were randomized into control and treatment groups when tumors reached the determined size of more than 0.2 cm3. Tumor volume (measured by caliper), animal body weight, and tumor condition were recorded twice weekly for the duration of the study. Tumor volume was calculated as described previously [1]. |
| 体外活性 | 方法：NRK-52E细胞用2.5,5,10,20μM AZD4547预处理1小时，然后暴露于0.5μg/ mLLPS指定时间，观察AZD4547对NRK-52E细胞中 LPS 诱导的炎症缺陷。 结果：AZD4547在NRK-52E细胞中以20μM的浓度显著抑制细胞增殖。[2] 方法：NRK-52E细胞用10μM AZD4547预处理1小时，然后暴露于0.5μg/ mL LPS指定时间，研究了 NRK-52E 细胞中促炎因子的水平。 结果：AZD4547通过减少NRK-52E细胞中的TAK1/NF-κB信号通路来减弱LPS诱导的炎症因子。[2] |
| 体内活性 | 方法：C57BL/6 小鼠使用LPS（15 mg/kg，腹膜内注射）并用AZD4547治疗（在LPS治疗前1小时灌胃40 mg/kg），研究 AZD4547 在 LPS 诱导的急性肾损伤中的肾保护作用以及测量了促凋亡基因Bax和抗凋亡基因Bcl-2研究AZD4547对AKI中保留肾功能的影响是否通过调节细胞凋亡来介导。 结果：AZD4547可以预防LPS相关的肾功能不全，细胞凋亡和小鼠肾脏炎症。[1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 252.5 mg/mL (544.69 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2.5 mg/mL (5.39 mM), Sonication is recommended. |
| 关键字 | KDR | Inhibitor | inhibit | Fibroblast growth factor receptor | FGFR4 | FGFR3 | FGFR2 | FGFR1 | FGFR | AZD-4547 | AZD4547 | AZD 4547 |
| 相关产品 | glycine | Amlexanox | Ribociclib | Lenvatinib | Chloramphenicol | Formononetin | Thymoquinone | Ferulic Acid | Regorafenib | Pazopanib | Sorafenib | Nintedanib esylate |
| 相关库 | Inhibitor Library | Angiogenesis related Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | NO PAINS Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 AZD4547【1035270-39-3】
￥226 - 2152
