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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Angiogenesis>Syk inhibitors>Fostamatinib Disodium
Fostamatinib Disodium
  • Fostamatinib Disodium

Fostamatinib Disodium NEW

Price $39 $50 $81
Package 1mg 2mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-17

Product Details

Product Name: Fostamatinib Disodium CAS No.: 1025687-58-4
Purity: 98.95% Supply Ability: 10g
Release date: 2024/11/17

Product Introduction

Bioactivity

名稱Fostamatinib Disodium
描述Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulatory activities.
細(xì)胞實驗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)
激酶實驗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.
體外活性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.
體內(nèi)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.
存儲條件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)
關(guān)鍵字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
相關(guān)產(chǎn)品UNC2025 | Gilteritinib | Fedratinib | Nintedanib | Sunitinib | Ellagic acid | Sunitinib Malate | Sorafenib | Tandutinib | ANTHRAQUINONE-2-CARBOXYLIC ACID | Pexidartinib | Sorafenib tosylate
相關(guān)庫經(jīng)典已知活性庫 | EMA 上市藥物庫 | 酪氨酸激酶分子庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抗病毒庫 | 抑制劑庫 | FDA 上市藥物庫 | FDA 上市激酶抑制劑庫 | 抗癌上市藥物庫 | 已知活性化合物庫

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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