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Fostamatinib Disodium

Catalog No. T2605 CAS 1025687-58-4

Synonyms: Tamatinib Fosdium, R788(Disodium), R788 Disodium, R788 (Fostamatinib) Disodium

Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulating activities.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Fostamatinib Disodium Chemical Structure

Fostamatinib Disodium, CAS 1025687-58-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 233.00
50 mg	In stock	$ 393.00
100 mg	In stock	$ 589.00
500 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 118.00

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Purity: 98.95%

Purity: 96.13%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulating activities.
Targets&IC50	Syk:41 nM
In vitro	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.
In vivo	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.
Kinase Assay	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.
Cell Research	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)

Synonyms	Tamatinib Fosdium, R788(Disodium), R788 Disodium, R788 (Fostamatinib) Disodium
Molecular Weight	624.42
Formula	C23H24FN6O9P·2Na
CAS No.	1025687-58-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 10 mM

References and Literature

1. Braselmann S, et al. J Pharmacol Exp Ther, 2006, 319(3), 998-1008. 2. Chen L, et al. Blood, 2008, 111(4), 2230-2237. 3. Suljagic M, et al. Blood, 2010, 116(23), 4894-4905.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Anti-Cancer Drug Library Clinical Compound Library FDA-Approved Drug Library Anti-Viral Compound Library

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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 Disodium 1025687-58-4 Angiogenesis Tyrosine Kinase/Adaptors Syk FLT FLT3 Tamatinib Fosdium Fms like tyrosine kinase 3 Spleen tyrosine kinase CD135 R-788 R788(Disodium) Fostamatinib R788 Disodium R788 (Fostamatinib) Disodium Cluster of differentiation antigen 135 inhibit R788 R 788 R788 (Fostamatinib) Inhibitor inhibitor

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