| 名称 | Fostamatinib Disodium |
| 描述 | Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulatory 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 | In mouse tumor models, daily administration of R935788 (80 mg/kg) effectively inhibited the growth of TCL1-002, TCL1-551, and TCL1-870 tumors. In Eμ-TCL1 transgenic mice, R935788 suppressed leukemia cell proliferation and survival by blocking antigen-dependent B-cell receptor signaling. |
| 体内活性 | R406, within a range of EC50 values (0.8-8.1 μM) across various diffuse large B-cell lymphoma cell lines, reduces the phosphorylation of BLNK, Akt, GSK-3, FOXO, and ERK, thereby inhibiting cell proliferation. |
| 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. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (80.07 mM)
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| 关键字 | FLT3 | Fms like tyrosine kinase 3 | Spleen tyrosine kinase | CD135 | R-788 | Fostamatinib | Fostamatinib Disodium | Syk | Cluster of differentiation antigen 135 | inhibit | R788 | R 788 | R788 (Fostamatinib) | Inhibitor |
| 相关产品 | UNC2025 | Gilteritinib | Fedratinib | Nintedanib | Sunitinib | Ellagic acid | Sunitinib Malate | Sorafenib | Tandutinib | ANTHRAQUINONE-2-CARBOXYLIC ACID | Pexidartinib | Sorafenib tosylate |
| 相关库 | 经典已知活性库 | EMA 上市药物库 | 酪氨酸激酶分子库 | 激酶抑制剂库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抗病毒库 | 抑制剂库 | FDA 上市药物库 | FDA 上市激酶抑制剂库 | 抗癌上市药物库 | 已知活性化合物库 |
United States
