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Fostamatinib

Fostamatinib
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Purity:98.3%
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Fostamatinib

Catalog No. T6115Cas No. 901119-35-5
Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
2 mg$52In Stock
5 mg$81In Stock
10 mg$120In Stock
25 mg$220In Stock
50 mg$353In Stock
100 mg$577In Stock
500 mg$1,260In Stock
1 mL x 10 mM (in DMSO)$103In Stock
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Product Introduction

Bioactivity
Description
Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.
In vitro
In rheumatoid arthritis models, Fostamatinib significantly reduces inflammatory mediators such as TNF-alpha, IL-1, IL-6, and IL-18, thereby diminishing inflammation and bone degeneration. It effectively inhibits BCR signaling in vivo, leading to decreased proliferation and survival of malignant B cells, and notably prolongs the survival of treated animals. Oral administration of Fostamatinib in reverse passive Arthus reaction and dual-antibody-induced arthritis mouse models reduces immune complex-mediated inflammation.
In vivo
In human adipocytes, macrophages, and neutrophils, Fostamatinib specifically inhibits FcγR signaling. It induces apoptosis in most DLBCL cell lines. Fostamatinib (EC50=56 nM) inhibits anti-IgE mediated CHMC degranulation in a dose-dependent manner. Additionally, it inhibits the production and release of LTC4, cytokines, and chemokines, including TNFα, IL-8, and GM-CSF, induced by anti-IgE.
Kinase Assay
Fluorescence polarization kinase assay and Ki determination: The fluorescence polarization reactions are performed. For Ki determination, duplicate 200-μL reactions are set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R788 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μL of each reaction is removed and quenched to stop the reaction. For each concentration of R788, the rate of reaction at each concentration of ATP is determined and plotted against the ATP concentration to determine the apparent Km and Vmax (maximal rate). Finally the apparent Km (or apparent Ki/Vmax) is plotted against the inhibitor concentration to determine the Ki.
Cell Research
Cultured human mast cells (CHMC) are derived from cord blood CD34+ progenitor cells and grown, primed, and stimulated and shown in supplemental data. Before stimulation, cells are incubated with R788 or DMSO for 30 minutes. Cells are then stimulated with either 0.25 to 2 mg/mL anti-IgE or anti-IgG or 2 μM ionomycin. For tryptase measurement, ∼1500 cells per well are stimulated for 30 min in modified Tyrode's buffer. For LTC4 and cytokine production, 100,000 cells per well are stimulated for 1 or 7 hours, respectively. Tryptase activity is measured by luminescence readout of a peptide substrate, and LTC4 and cytokines are measured using Luminex multiplex technology. (Only for Reference)
AliasR788
Chemical Properties
Molecular Weight580.46
FormulaC23H26FN6O9P
Cas No.901119-35-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 107 mg/mL (184.3 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7228 mL8.6139 mL17.2277 mL86.1386 mL
5 mM0.3446 mL1.7228 mL3.4455 mL17.2277 mL
10 mM0.1723 mL0.8614 mL1.7228 mL8.6139 mL
20 mM0.0861 mL0.4307 mL0.8614 mL4.3069 mL
50 mM0.0345 mL0.1723 mL0.3446 mL1.7228 mL
100 mM0.0172 mL0.0861 mL0.1723 mL0.8614 mL

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