Fostamatinib Disodium

SKU: orb1305272

Description

Fostamatinib Disodium (R788 Disodium) is an orally bioavailable inhibitor of spleen tyrosine kinase (Syk). It is used in research to investigate immunomodulation and inflammation, with applications in both in vitro cellular assays and in vivo models of autoimmune and hematologic disorders.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1025687-58-4
• MW: 624.42
• Purity: 99.09%
• Formula: C₂₃H₂₄FN₆O₉P·2Na
• SMILES: [Na+].[Na+].COc1cc(Nc2ncc(F)c(Nc3ccc4OC(C)(C)C(=O)N(COP([O-])([O-])=O)c4n3)n2)cc(OC)c1OC
• Target: FLT,Syk
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.2 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:50 mg/mL (80.07 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Syk:41 nM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: 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/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CD135, Cluster of differentiation antigen 135, Inhibitor, Fostamatinib, Fostamatinib Disodium, Fms like tyrosine kinase 3, FLT3, inhibit, Tamatinib Fosdium, Syk, Spleen tyrosine kinase, R 788, R788 (Fostamatinib), R788 (Fostamatinib) Disodium, R788 Disodium, R788(Disodium), R788, R-788

Compound Identifiers

PubChem CID

25008120