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Purity: ≥98%
Fostamatinib (formerly also known as R788; trade name: Tavalisse), a prodrug of the active metabolite R406, is an orally bioactive, potent and selective Syk inhibitor with potential anti-inflammatory activity. It inhibits Syk with an IC50 of 41 nM in a cell-free assay. On April 17th 2018, Fostamatinib was approved by the US FDA for the treatment of thrombocytopenia in adult patients with persistent or chronic immune thrombocytopenia (ITP).
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In Louvain rats, fostamatinib (R788) is highly bioavailable and rapidly absorbed. AUC0–16 hours were 10618 ng*h/mL and 30650 ng*h/mL, respectively; Cmax=2600 ng/mL and 6500 ng/mL (1 hour observation); t1/2=4.2 hours were recorded in R406 following a single oral dosage of R788 10 mg/kg or 20 mg/kg. The absence of prodrug in plasma suggests that R788 has fully transformed into R406 [1].
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| References |
[1]. Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273.
[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. [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. |
| Molecular Formula |
C23H26FN6O9P
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| Molecular Weight |
580.46
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| CAS # |
901119-35-5
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| Related CAS # |
Fostamatinib Disodium;1025687-58-4;Fostamatinib disodium hexahydrate;914295-16-2
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| 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
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4% DMSO+30% PEG 300+ddH2O:5 mg/mL Solubility in Formulation 5: 10 mg/mL (17.23 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; Need ultrasonic and warming and heat to 40°C. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1723 mL | 0.8614 mL | 1.7228 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05904093 | Not yet recruiting | Drug: Fostamatinib | Sickle Cell Disease Hb-SS Disease |
National Heart, Lung, and Blood Institute (NHLBI) |
April 16, 2024 | Phase 1 |
| NCT04543279 | Terminated | Drug: Fostamatinib Drug: Ruxolitinib |
Myelofibrosis Thrombocytopenia |
Washington University School of Medicine |
May 3, 2021 | Phase 2 |
| NCT03246074 | Active,not recruiting | Drug: Fostamatinib and Paclitaxel |
Ovarian Cancer | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins |
April 3, 2018 | Phase 1 |
| NCT05509582 | Enrolling by invitation | Drug: fostamatinib | Immune Mediated Anemia | National Heart, Lung, and Blood Institute (NHLBI) |
April 16, 2024 | Phase 2 |
| NCT03991780 | Recruiting | Drug: Fostamatinib | Renal Transplant Rejection | Imperial College London | May 8, 2019 | Phase 1 Phase 2 |
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