Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD4547 是FGFR 家族抑制剂,能够作用于FGFR1 (IC50:0.2 nM),FGFR2 (IC50:2.5 nM),FGFR3 (IC50:1.8 nM) 和FGFR4 (IC50:165 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 263 | 现货 | ||
2 mg | ¥ 371 | 现货 | ||
5 mg | ¥ 617 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,390 | 现货 | ||
50 mg | ¥ 2,320 | 现货 | ||
100 mg | ¥ 3,730 | 现货 | ||
200 mg | ¥ 5,420 | 现货 | ||
500 mg | ¥ 8,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 678 | 现货 |
产品描述 | AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays). |
靶点活性 | FGFR3:1.8 nM (cell free), FGFR1:0.9 nM (cell free), KDR:24 nM (cell free), FGFR2:2.5 nM (cell free) |
体外活性 | AZD4547 potently inhibits the tyrosine kinase activities of recombinant FGFR1/2/3 in vitro (IC50s: 0.2/2.5/1.8 nmol/L) and displays weaker activity against FGFR4 (IC50: 165 nmol/L). AZD4547 shown to inhibit recombinant VEGFR2 (KDR) kinase activity (IC50: 24 nmol/L). AZD4547 inhibited the proliferation of KG1a cells and KMS11 cells (IC50s: 18 and 281 nmol/L). Notably, MCF7 cell proliferation was unaffected by incubation with AZD4547 up to a concentration of 30 μmol/L [1]. Of 78 cell lines, only 2 (DMS114 and NCI-H1581) displayed a profound sensitivity to AZD4547, with GI50 values of 0.111 and 0.003 μmol/L, respectively [2]. |
体内活性 | Twice daily administration of AZD4547 at 3 mg/kg gave statistically significant tumor growth inhibition of 53% when compared with vehicle-treated controls, whereas doses of 12.5 mg/kg once daily and 6.25 mg/kg twice daily resulted in complete tumor stasis. A further efficacy study in the KG1a model with 12.5 mg/kg once daily AZD4547 resulted in 65% tumor growth inhibition [1]. Tumor-bearing mice were randomly grouped and dosed orally, once daily with vehicle, 3.125, 6.25, or 12.5 mg/kg AZD4547 for a period of 15 days. Potent tumor regressions were observed in the 6.25 and 12.5 mg/kg treatment groups, whereas tumor stasis followed by slow regrowth was observed in the 3.125 mg/kg treatment group [2]. |
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]. |
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]. |
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]. |
分子量 | 463.57 |
分子式 | C26H33N5O3 |
CAS No. | 1035270-39-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 85 mg/mL (183.4 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1572 mL | 10.7859 mL | 21.5717 mL | 53.9293 mL |
5 mM | 0.4314 mL | 2.1572 mL | 4.3143 mL | 10.7859 mL | |
10 mM | 0.2157 mL | 1.0786 mL | 2.1572 mL | 5.3929 mL | |
20 mM | 0.1079 mL | 0.5393 mL | 1.0786 mL | 2.6965 mL | |
50 mM | 0.0431 mL | 0.2157 mL | 0.4314 mL | 1.0786 mL | |
100 mM | 0.0216 mL | 0.1079 mL | 0.2157 mL | 0.5393 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AZD4547 1035270-39-3 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR Inhibitor Fibroblast growth factor receptor AZD 4547 inhibit AZD-4547 inhibitor