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- 文献和实验
- 技术资料
- CAS号：
1025687-58-4
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥904.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥233.0 |
| 规格： | 2mg | 产品价格： | ￥332.0 |
| 规格： | 5mg | 产品价格： | ￥662.0 |
| 规格： | 10mg | 产品价格： | ￥1064.0 |
| 规格： | 25mg | 产品价格： | ￥1880.0 |
| 规格： | 50mg | 产品价格： | ￥2984.0 |
| 规格： | 100mg | 产品价格： | ￥4360.0 |
Product Introduction
Bioactivity
| 名称 | Fostamatinib Disodium |
| 描述 | Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulating activities. |
| 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) |
| 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. |
| 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。 |
| 存储条件 | Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 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 mg/mL (3.2 mM), Sonication is recommended. DMSO : 50 mg/mL (80.07 mM), Sonication is recommended. |
| 关键字 | Syk | Spleen tyrosine kinase | R788 (Fostamatinib) | R-788 | R788 | R 788 | Inhibitor | inhibit | Fostamatinib Disodium | Fostamatinib | Fms like tyrosine kinase 3 | FLT3 | Cluster of differentiation antigen 135 | CD135 |
| 相关产品 | Onatasertib | Gilteritinib | Fostamatinib | ANTHRAQUINONE-2-CARBOXYLIC ACID | Ellagic acid | Quizartinib | Nintedanib | Sorafenib | Pexidartinib | Sunitinib | Brigatinib | Ripretinib |
| 相关库 | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | FDA-Approved Drug Library | Anti-Viral Compound Library | Immunology/Inflammation Compound Library | Membrane Protein-targeted Compound Library | FDA-Approved Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library |
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手套、面罩，并且在通风橱内操作。 4.2 10XTNE储存缓冲液 溶解于800ml蒸馏水中：12.11g Tris碱[Tris（羟甲基）氨基甲烷]，分子量=121.14；3.72g EDTA乙二胺四乙酸，二钠盐，二水合物，分子量=372.20；116.89g 氯化钠，分子量=58.44。用浓盐酸调节溶液PH至7.4，补加蒸馏水定容至1000ml，使用前用0.45μm滤膜过滤，4℃可保存3个月。 注
盐 57.66 57 胸腺嘧啶 0.300 28 DL-缬氨酸 50.00 58
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福他替尼二钠盐【1025687-58-4】
￥233 - 4360
