2. Protein Tyrosine Kinase/RTK
  3. Syk FLT3
  4. Fostamatinib

Fostamatinib (R788) is the oral proagent of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).

For research use only. We do not sell to patients.

CAS No. : 901119-35-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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1 mg In-stock
5 mg In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Fostamatinib:

Fostamatinib Related Antibodies

Top Publications Citing Use of Products

    Fostamatinib purchased from MedChemExpress. Usage Cited in: BMC Med. 2024 Mar 5;22(1):96.  [Abstract]

    CCK-8 assay showed that Fostamatinib (R788, 1.25–20 μM; 5 h) exhibited mild cytotoxicity in a dose-dependent manner.

    Fostamatinib purchased from MedChemExpress. Usage Cited in: BMC Med. 2024 Mar 5;22(1):96.  [Abstract]

    Western blotting analysis of p-p65, p-IRF3, and p-TBK1 from THP-1 cells subjected to MSA-2 stimulation and treated with Fostamatini (R788, 10–20 μM) or AMX (100–200 μM). The results showed that R788 significantly inhibited the levels of phosphorylated TBK1 (p-TBK1) and IRF3 (p-IRF3), with no effect on p65 phosphorylation (p-p65), indicating the specific inhibition on TBK1 within TBK1/IRF3 signaling pathway.

    Fostamatinib purchased from MedChemExpress. Usage Cited in: BMC Med. 2024 Mar 5;22(1):96.  [Abstract]

    RT-qPCR showed the relative levels (normalized with GAPDH) of IFNB, TNFA, and IL6 from NSC-34 cells treated with Fostamatinib (R788, 1.25–20 μM).

    Fostamatinib purchased from MedChemExpress. Usage Cited in: Gene. 2020 Jun 20;744:144608.  [Abstract]

    Cell Counting Kit-8 assay results showing the effect of Fostamatinib (10 μM) on the proliferative capacity of PC-3 cells.

    Fostamatinib purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2014 Aug 22;4(8):e240.  [Abstract]

    Hematoxylin and eosin-stained liver slides and reticulin stained BM slides are shown from one Fostamatinib (R788, 40 mg/kg; oral gavage; twice daily) treated mouse versus control mouse. Arrows show liver infiltrates in the control group, which are absent in the treatment group. The results showed that in the Fostamatinib (R788, 40 mg/kg; oral gavage; twice daily) group, virtually no infiltration of granulocyte and megakaryocyte progenitor cells was observed in the liver.

    Fostamatinib purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2014 Aug 22;4(8):e240.  [Abstract]

    Fostamatinib (R788, 40 mg/kg; oral gavage; twice a day) significantly improved the survival rate of Balb/c mice transplanted with the TEL‑SYK oncogene by inhibiting SYK (Fig. a), effectively reduced the sizes of the spleen and liver (Fig. b), and decreased white blood cell (WBC) counts simultaneously (Fig. c).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fostamatinib (R788) is the oral proagent of the active compound R406[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM[2]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[3].

    IC50 & Target

    Syk, FLT3[2]
    Cellular Effect
    Cell Line Type Value Description References
    Ramos IC50
    0.267 μM
    Compound: 1
    Inhibition of SYK in human Ramos cells
    Inhibition of SYK in human Ramos cells
    		[PMID: 23350847]
    In Vivo

    Fostamatinib (R788) is highly bioavailable, and rapidly absorbed in Louvain rats. R406 following a single oral dose of R788 10 mg/kg or 20 mg/kg: AUC0-16 hrs= 10618 ng*h/mL and 30650 ng*h/mL respectively; Cmax=2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour); t1/2=4.2 hours. The prodrug was not detected in plasma suggesting R788 is completely converted to R406[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    580.46

    Formula

    C23H26FN6O9P
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O)(O)=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (107.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7228 mL 8.6139 mL 17.2277 mL
    5 mM 0.3446 mL 1.7228 mL 3.4455 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    C2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (3.58 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (17.23 mM); Suspended solution; Need ultrasonic and warming and heat to 40°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.70%

    SDS (393 KB)

    COA (250 KB) HNMR (140 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7228 mL 8.6139 mL 17.2277 mL 43.0693 mL
    5 mM 0.3446 mL 1.7228 mL 3.4455 mL 8.6139 mL
    10 mM 0.1723 mL 0.8614 mL 1.7228 mL 4.3069 mL
    15 mM 0.1149 mL 0.5743 mL 1.1485 mL 2.8713 mL
    20 mM 0.0861 mL 0.4307 mL 0.8614 mL 2.1535 mL
    25 mM 0.0689 mL 0.3446 mL 0.6891 mL 1.7228 mL
    30 mM 0.0574 mL 0.2871 mL 0.5743 mL 1.4356 mL
    40 mM 0.0431 mL 0.2153 mL 0.4307 mL 1.0767 mL
    50 mM 0.0345 mL 0.1723 mL 0.3446 mL 0.8614 mL
    60 mM 0.0287 mL 0.1436 mL 0.2871 mL 0.7178 mL
    80 mM 0.0215 mL 0.1077 mL 0.2153 mL 0.5384 mL
    100 mM 0.0172 mL 0.0861 mL 0.1723 mL 0.4307 mL
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    Fostamatinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Fostamatinib901119-35-5R788R 788R-788SykFLT3Spleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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