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

Fostamatinib Disodium  (Synonyms: R788(Disodium))

Cat. No.: HY-13038 Purity: 99.88%
Data Sheet
SDS
COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

Fostamatinib Disodium (R788 Disodium) 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.

Fostamatinib Disodium Chemical Structure

Fostamatinib Disodium Chemical Structure

CAS No. : 1025687-58-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 146 In-stock
Solution
10 mM * 1 mL in DMSO USD 153 In-stock
Solid
1 mg USD 53 In-stock
5 mg USD 111 In-stock
10 mg USD 166 In-stock
50 mg USD 499 In-stock
100 mg USD 818 In-stock
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500 mg   Get quote  

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Fostamatinib Disodium:

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  • Purity & Documentation

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Description

Fostamatinib Disodium (R788 Disodium) 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]
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
NCT NumberSponsorConditionStart DatePhase
NCT01197521AstraZeneca
Rheumatoid Arthritis
September 2010Phase 3
NCT01563978AstraZeneca
Rheumatoid Arthritis
April 2012Phase 2
NCT02076412Rigel Pharmaceuticals
Immune Thrombocytopenic Purpura
January 2015Phase 3
Molecular Weight

624.42

Formula

C23H24FN6Na2O9P
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (33.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 1 mg/mL (1.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6015 mL 8.0074 mL 16.0149 mL
5 mM 0.3203 mL 1.6015 mL 3.2030 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (4.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.88%

Data Sheet (275 KB) SDS (252 KB)

COA (250 KB)LCMS (107 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.6015 mL 8.0074 mL 16.0149 mL 40.0372 mL
DMSO 5 mM 0.3203 mL 1.6015 mL 3.2030 mL 8.0074 mL
10 mM 0.1601 mL 0.8007 mL 1.6015 mL 4.0037 mL
15 mM 0.1068 mL 0.5338 mL 1.0677 mL 2.6691 mL
20 mM 0.0801 mL 0.4004 mL 0.8007 mL 2.0019 mL
25 mM 0.0641 mL 0.3203 mL 0.6406 mL 1.6015 mL
30 mM 0.0534 mL 0.2669 mL 0.5338 mL 1.3346 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Fostamatinib Disodium Related Classifications

Keywords:

Fostamatinib Disodium1025687-58-4R788(Disodium)SykFLT3Spleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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