Cat. No.: HY-13038A

Fostamatinib

(Synonyms: R788)

16 Cited Publications

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Based on 16 publication(s) in Google Scholar

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

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Pureté: 99.70%
CAS No.: 901119-35-5
Formule: C₂₃H₂₆FN₆O₉P
Masse moléculaire:580.46

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Fostamatinib Chemical Structure

CAS No.: 901119-35-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Essai clinique
Chemical Information
Publications (16)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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 K_i 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: AUC_{0-16 hrs}= 10618 ng*h/mL and 30650 ng*h/mL respectively; C_max=2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour); t_1/2=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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 901119-35-5
Appearance Solid
Masse moléculaire 580.46
Formule C₂₃H₂₆FN₆O₉P
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
Synonyms

R788
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (16)

All Histological Imaging/StainingIn Vivo Efficacy StudyCell Proliferation/Viability AssayWBRT-PCR

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Journal Impact Factor

Cancer Cell

SYK is a critical regulator of FLT3 in acute myeloid leukemia. [Abstract]

2014 Feb 10;25(2):226-42. PMID: 24525236
Nat Med

Macrophage extracellular trap formation promoted by platelet activation is a key mediator of rhabdomyolysis-induced acute kidney injury. [Abstract]

2018 Feb;24(2):232-238. PMID: 29309057
Blood

2022 Nov 15.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Blood Cancer J

Depletion of STAT5 blocks TEL-SYK-induced APMF-type leukemia with myelofibrosis and myelodysplasia in mice. [Abstract]

2014 Aug 22;4(8):e240. PMID: 25148222

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).
BMC Med

TBK1, a prioritized drug repurposing target for amyotrophic lateral sclerosis: evidence from druggable genome Mendelian randomization and pharmacological verification in vitro. [Abstract]

2024 Mar 5;22(1):96. PMID: 38443977

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).
EMBO J

Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2 S production. [Abstract]

2021 Jun 1;40(11):e106771. PMID: 33909912
Br J Cancer

Circulating tumour cell-derived xenograft as a preclinical platform for metastatic breast cancer. [Abstract]

2026 May 18. PMID: 42151560
Biomedicines

SIK2 Drives Pulmonary Fibrosis by Enhancing Fibroblast Glycolysis and Activation. [Abstract]

2025 Aug 6;13(8):1919. PMID: 40868174
Mol Divers

Exploiting the Achilles' heel of cancer through a structure-based drug-repurposing approach and experimental validation of top drugs using the TRAP assay. [Abstract]

2025 Mar 14. PMID: 40087255
Hematol Oncol

Gene Expression Profiling in Acute Myeloid Leukemia Patient Subgroups With High and Low Sensitivity Toward SYK Inhibitors. [Abstract]

2025 Mar;43(2):e70058. PMID: 40088478
Metabolomics

2026 Apr 17;22(3):51.
Gene

PKMYT1 is associated with prostate cancer malignancy and may serve as a therapeutic target. [Abstract]

2020 Jun 20:744:144608. PMID: 32234541

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.
Patent

US20230288401A1.
Research Square Print

2023 Mar 17.
Oxid Med Cell Longev

Resveratrol Confers Vascular Protection by Suppressing TLR4/Syk/NLRP3 Signaling in Oxidized Low-Density Lipoprotein-Activated Platelets. [Abstract]

2021 Feb 25:2021:8819231. PMID: 33728029

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7228 mL

8.6139 mL

17.2277 mL

5 mM

0.3446 mL

1.7228 mL

3.4455 mL

10 mM

0.1723 mL

0.8614 mL

1.7228 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273. [Content Brief]

[2]. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. [Content Brief]

[3]. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Fostamatinib

16 Cited Publications

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Fostamatinib

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Publications Citing Use of MedChemExpress (MCE) Fostamatinib

Activité biologique

Chemical Information

Publications (16)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fostamatinib Related Classifications

HY-13038A Related Classifications