Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tyrphostin AG1296 (Tyrphostin AG 1296) 抑制人PDGF α和β受体以及相关干细胞因子受体的信号传导,是一种选择性血小板衍生生长因子受体抑制剂,IC50值为 0.8 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
2 mg | ¥ 483 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,380 | 现货 | ||
25 mg | ¥ 2,490 | 现货 | ||
50 mg | ¥ 3,590 | 现货 | ||
100 mg | ¥ 5,130 | 现货 | ||
500 mg | ¥ 10,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 938 | 现货 |
产品描述 | Tyrphostin AG1296 (Tyrphostin AG 1296) is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. |
靶点活性 | c-Kit (Swiss 3T3):1.8 μM, FGFR (Swiss 3T3):12.3 μM, PDGFR:0.3 μM-0.5 μM |
体外活性 | AG 1296 inhibits selectively the PDGF receptor kinase and the PDGF dependent DNA synthesis in Swiss 3T3 cells and in porcine aorta endothellal cells with 50% inhibitory concentrations below 5 and 1μM, respectively. AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. AG1296 potently inhibits signaling of human PDGF -α and -β receptors but has no effect on autophosphorylation of the VEGFR KDR or on DNA synthesis induced by VEGF in porcine aortlc endothelial cells. Treatment by AG1296 reverses the transformed phenotype of sis-transfected NIH 3T3 cells but has no effect on src-transformed NIH3T3 cells.AG1296 is an ATP-competitive inhibitor. AG1296 interferes neither with PDGF binding nor with PDGF receptor dimerization while it abolishes PDGF receptor autophosphorylation. Thus, AG1296 is a pure inhibitor of the catalytic activity of the receptor tyrosine kinase. |
激酶实验 | Membrane Autophosphorylation Assays:Membranes are prepared from confluent cultures of Swiss 3T3 cells as described. For measuring receptor autophosphorylation, 10μg membrane protein per assay are incubated for 20 min on ice in the presence of 1.2μg/mL EGF or 2μg/mL PDGF, or both; 50 mM Hepes (pH 7.5); and 3 mM MnCl2 in a volume of 45μl. In order to test the effects of tyrphostins, these are added in a volume of 0.5 μl (in DMSO; final concentration, 0.5%) 15 min before addition of the growth factors. Phosphorylation is initiated by addition of [γ-32P]ATP and terminated after 2 min by addition of 10μL of a solution containing 6% SDS, 30%β-mercatoethanol, 40% glycerol, and 0.5 mg/mL bromophenol blue. The samples are heated for 5 min at 95 ℃ and subjected to SDS-PAGE using 10% acrylamide gels. The gels are stained and dried and subjected to autoradiographic analysis. |
细胞实验 | Cell lines: Swiss 3T3. Concentrations: ~50 μM. Incubation Time: 3 days. Method: Cells are seeded in 24-well plates (5000 cells/well) in DMEM/10% FCS.On the next day the medium is changed to DMEM/2% FcS with or without growth factors and tyrphostins are added as indicated.Three days later the cells are counted in a hemocytometer |
别名 | Tyrphostin AG 1296, AG 1296 |
分子量 | 266.29 |
分子式 | C16H14N2O2 |
CAS No. | 146535-11-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 6 mg/mL (22.53 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 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 | 3.7553 mL | 18.7765 mL | 37.553 mL | 93.8826 mL |
5 mM | 0.7511 mL | 3.7553 mL | 7.5106 mL | 18.7765 mL | |
10 mM | 0.3755 mL | 1.8777 mL | 3.7553 mL | 9.3883 mL | |
20 mM | 0.1878 mL | 0.9388 mL | 1.8777 mL | 4.6941 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。
Tyrphostin AG1296 146535-11-7 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FGFR FLT PDGFR c-Kit Fms like tyrosine kinase 3 PDGF AG-1296 CD117 inhibit platelet-derived CD135 SCFR Tyrphostin AG-1296 FLT3 cell growth stem Inhibitor Cluster of differentiation antigen 135 Tyrphostin AG 1296 AG 1296 factor Platelet-derived growth factor receptor AG1296 inhibitor