Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fostamatinib Disodium (R788 Disodium) 是一种口服具有活力的 R406 前药。其中R406 是具有口服活性的,有效的,ATP 竞争性的Syk/FLT3抑制剂(Ki:30 nM,IC50:41 nM),也能够抑制 Lyn (IC50:63 nM) 和 Lck (IC50:37 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 272 | 现货 | ||
2 mg | ¥ 415 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,350 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,450 | 现货 | ||
500 mg | ¥ 11,300 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulating activities. |
靶点活性 | Syk:41 nM |
体外活性 | 在小鼠肿瘤模型中,每天R935788(80 mg/kg)能够有效抑制 TCL1-002, TCL1-551 和 TCL1-870肿瘤生长.在Eμ-TCL1转基因小鼠中,R935788通过阻止抗原依赖性B细胞受体的信号,抑制白血病细胞增殖和存活. |
体内活性 | 在多种弥散性大B细胞淋巴瘤细胞系中(EC50=0.8-8.1 μM),R406降低BLNK, Akt, GSK-3, FOXO和ERK 磷酸化,抑制细胞增殖。 |
激酶实验 | In vitro fluorescence polarization kinase assays: R406 (in vitro active form of R935788) is serially diluted in DMSO and then diluted to 1% DMSO in kinase buffer (20 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM MnCl2, 1 mM DTT, 0.1 mg/mL acetylated BGG). ATP and substrate in kinase buffer are added at room temperature, resulting in a final DMSO concentration on 0.2%. The kinase reactions are performed in a final volume of 20 μL containing 5 μM HS1 peptide substrate and 4 μM ATP and started by addition of 0.125 ng of Syk in kinase buffer. The reaction is allowed to proceed for 40 minutes at room temperature. The reaction is stopped by the addition of 20 μL of PTK quench mix containing EDTA/anti-phosphotyrosine antibody (1× final)/fluorescent phosphopeptide tracer (0.5× final) diluted in FP Dilution Buffer. The plate is incubated for 30 minutes in the dark at room temperature and then read on a Polarion fluorescence polarization plate reader. Data is converted to determine the amount of phosphopeptide present using a calibration curve generated by competition with the phosphopeptide competitor provided in the Tyrosine Kinase Assay Kit. For IC50 determination, R406 is tested at eleven concentrations in duplicate and curve-fitting is performed by non-linear regression analysis using Prism GraphPad Software. |
细胞实验 | Cells are exposed to increasing concentrations of R406 (in vitro active form of R935788) for 48 hours. The percentage of apoptotic cells is determined by double staining with propidium iodide (PI) and annexin-A5–FITC conjugate. Ki-67 staining is performed with the FITC mouse anti–Ki-67 set. Samples are analyzed on a FACSCalibur flow cytometer with CellQuest Version 3.3 software. (Only for Reference) |
别名 | Tamatinib Fosdium, 福他替尼二钠盐, R788(Disodium), R788 Disodium, R788 (Fostamatinib) Disodium |
分子量 | 624.42 |
分子式 | C23H24FN6O9P·2Na |
CAS No. | 1025687-58-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 10 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6015 mL | 8.0074 mL | 16.0149 mL | 40.0372 mL |
5 mM | 0.3203 mL | 1.6015 mL | 3.203 mL | 8.0074 mL | |
10 mM | 0.1601 mL | 0.8007 mL | 1.6015 mL | 4.0037 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。
Fostamatinib Disodium 1025687-58-4 Angiogenesis Tyrosine Kinase/Adaptors FLT Syk FLT3 Tamatinib Fosdium Fms like tyrosine kinase 3 Spleen tyrosine kinase 福他替尼二钠盐 CD135 R-788 R788(Disodium) Fostamatinib R788 Disodium R788 (Fostamatinib) Disodium Cluster of differentiation antigen 135 inhibit R788 R 788 R788 (Fostamatinib) Inhibitor inhibitor