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Fostamatinib

Catalog No. T6115 CAS 901119-35-5

Synonyms: R788, 福他替尼

Fostamatinib(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.

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Fostamatinib, CAS 901119-35-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Fostamatinib(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.
Targets&IC50	Syk:41 nM
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, &sim;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)

Synonyms	R788, 福他替尼
Molecular Weight	580.466
Formula	C23H26FN6O9P
CAS No.	901119-35-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

Ethanol: <1 mg/mL

DMSO: 107 mg/mL (184.3 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Braselmann S, et al. J Pharmacol Exp Ther, 2006, 319(3), 1998-12008. 2. Chen L et al.Blood, 2008, 111(4), 2230-2237. 3. Suljagic M, et al. Blood, 2010, 116(23), 4894-4905. 4. Bajpai M. IDrugs, 2009, 12(3), 174-185.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library GPCR Compound Library Neurotransmitter Receptor Compound Library Drug-induced Liver Injury (DILI) Compound Library Ion Channel Inhibitor Library Immunology/Inflammation Compound Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library FDA-Approved Drug Library

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Related compounds with same targets

GR79236 A2A receptor antagonist 1 ST-1535 GW-493838 ANR 94 2-Ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridine Nelonicline PF-02575799

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Fostamatinib 901119-35-5 G蛋白偶联受体蛋白酪氨酸激酶离子通道神经科学血管生成 Adenosine Receptor FLT Monoamine Transporter Syk Inhibitor R 788 Spleen tyrosine kinase Cluster of differentiation antigen 135 R-788 Fms like tyrosine kinase 3 CD135 inhibit R788 FLT3 inhibitor

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