Fostamatinib (R788)

Catalog No.S2625

Fostamatinib (R788) Chemical Structure

Molecular Weight(MW): 580.46

Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.

Size Price Stock Quantity  
In DMSO USD 650 In stock
USD 270 In stock
USD 470 In stock
USD 870 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

  • B cells were stimulated by irradiated CD40L+ L cells. Forward scatter vs. BrdU incorporation analysis (day 5) in the gated CD19+ CLL cells (D). The distribution of cells with high FSC (blasts, right quadrants) and proliferation (BrdU+, upper quadrants) are shown.

    Haematologica, 2016 Feb, 101(2): e59–e62.. Fostamatinib (R788) purchased from Selleck.

Purity & Quality Control

Choose Selective Syk Inhibitors

Biological Activity

Description Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.
Features Converted into its active metabolite R406 in vivo.
Targets
Syk [1] Adenosine A3 receptor [1] Adenosine transporter [1] Monoamine transporter [1]
41 nM 81 nM 1.84 μM 2.74 μM
In vitro

R788 is a prodrug of the spleen tyrosine kinase (Syk) inhibitor R406. R788 is a competitive inhibitor for ATP binding with a Ki of 30 nM. R788 dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM. R788 also inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. Inhibition of Syk by R788 results in inhibition of all phosphorylation events downstream of Syk signaling. Next to FcϵRI signaling in CHMC, R788 most potently inhibits the signaling of IL-4 and IL-2 receptors. R788 specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils. R788 can inhibit local inflammatory injury mediated by immune complexes. [1] R788 induces apoptosis of the majority of examined DLBCL cell lines. In R788-sensitive DLBCL cell lines, R788 specifically inhibits both tonic- and ligand-induced BCR signaling (autophosphorylation of SYK525/526 and SYK-dependent phosphorylation of the B-cell linker protein [BLNK]). [2]

In vivo Oral administration of R788 to mice reduces immune complex-mediated inflammation in a reverse-passive Arthus reaction and two antibody-induced arthritis models. [1] In another study, R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolongs survival of the treated animals. [3] R788 demonstrates a significant reduction in major inflammatory mediators such as TNFalpha, IL-1, IL-6 and IL-18, leading to reduced inflammation and bone degradation in models of rheumatoid arthritis. [4]

Protocol

Kinase Assay:

[1]

+ Expand

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:

[1]

+ Expand
  • Cell lines: Cultured human mast cells (CHMC)
  • Concentrations: 0 μM -100 μM
  • Incubation Time: 30 minutes
  • Method:

    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)
Animal Research:

[1]

+ Expand
  • Animal Models: Balb/c mice with arthritis
  • Formulation: 35% TPGS, 60% PEG 400, 5% propylene glycol
  • Dosages: 1 mg/kg or 5 mg/kg
  • Administration: Orally b.i.d
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 116 mg/mL (199.84 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
4% DMSO+30% PEG 300+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 580.46
Formula

C23H26FN6O9P

CAS No. 901119-35-5
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02612558 Recruiting Warm Antibody Autoimmune Hemolytic Anemia Rigel Pharmaceuticals April 2016 Phase 2
NCT02611063 Recruiting Hematological Malignancies Stefanie Sarantopoulos, MD, PhD.|Duke University January 2016 Phase 1
NCT02433236 Withdrawn IGA Nephropathy Rigel Pharmaceuticals September 2015 Phase 2
NCT02076412 Completed Immune Thrombocytopenic Purpura Rigel Pharmaceuticals November 2014 Phase 3
NCT02112838 Recruiting IGA Nephropathy Rigel Pharmaceuticals October 2014 Phase 2
NCT02077192 Recruiting Immune Thrombocytopenic Purpura Rigel Pharmaceuticals July 2014 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Syk Signaling Pathway Map

Syk Inhibitors with Unique Features

Related Syk Products

Tags: buy Fostamatinib (R788) | Fostamatinib (R788) supplier | purchase Fostamatinib (R788) | Fostamatinib (R788) cost | Fostamatinib (R788) manufacturer | order Fostamatinib (R788) | Fostamatinib (R788) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID