Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Fostamatinib disodium (also known as R-788; R-935788; brand name: Tavalisse) is the prodrug form of the active metabolite R406. It is an orally bioactive and selective Syk inhibitor with anti-inflammatory activity. It inhibits Syk kinase with IC50 of 41 nM in a cell-free assay. As of 2018, Fostamatinib gained FDA approval to treat thrombocytopenia in adult patients with persistent or chronic immune thrombocytopenia (ITP). Fostamatinib strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Fostamatinib has displayed anti-inflammatory and immunomodulating activities.
ln Vitro |
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ln Vivo |
In Louvain rats, fostamatinib (R788) is highly bioavailable and rapidly absorbed. Following a single oral dose of R788 10 mg/kg or R406 20 mg/kg, the following results were observed after one hour: t1/2 = 4.2 hours; AUC0-16 hrs = 10618 ng*h/mL and 30650 ng*h/mL, respectively; Cmax = 2600 ng/mL and 6500 ng/mL, respectively. The complete conversion of R788 to R406 was shown by the absence of prodrug in plasma [1].
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Animal Protocol |
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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 |
C23H24FN6NA2O9P
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Molecular Weight |
624.42
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CAS # |
1025687-58-4
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Related CAS # |
Fostamatinib;901119-35-5;Fostamatinib disodium hexahydrate;914295-16-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=P([O-])([O-])OCN1C2=NC(NC3=NC(NC4=CC(OC)=C(OC)C(OC)=C4)=NC=C3F)=CC=C2OC(C)(C)C1=O.[Na+].[Na+]
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InChi Key |
HSYBQXDGYCYSGA-UHFFFAOYSA-L
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InChi Code |
InChI=1S/C23H26FN6O9P.2Na/c1-23(2)21(31)30(11-38-40(32,33)34)20-14(39-23)6-7-17(28-20)27-19-13(24)10-25-22(29-19)26-12-8-15(35-3)18(37-5)16(9-12)36-4;;/h6-10H,11H2,1-5H3,(H2,32,33,34)(H2,25,26,27,28,29);;/q;2*+1/p-2
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Chemical Name |
sodium (6-((5-fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate
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Synonyms |
Fostamatinib disodium hexahydrate; R788; R 788; R-788 sodium; Tamatinib Fosdium, R-935788; R935788; R-935788; R 935788; R935788 sodium. Fostamatinib sodium, prodrug of R-406.
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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: ≥ 2.5 mg/mL (4.00 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 25.0 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: ≥ 2.5 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 0.5% CMC+0.25% Tween 80,pH6.5:30 mg/mL |
Preparing Stock Solutions | 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 | |
10 mM | 0.1601 mL | 0.8007 mL | 1.6015 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 |
NCT00798096 | Completed Has Results | Drug: Fostamatinib Disodium | T Cell Lymphoma | Rigel Pharmaceuticals | March 2009 | Phase 2 |
NCT00923481 | Completed Has Results | Drug: Fostamatinib disodium | Head and Neck Neoplasms Pheochromocytoma |
National Cancer Institute (NCI) | April 2009 | Phase 2 |
NCT02077192 | Completed Has Results | Drug: Fostamatinib Disodium | Immune Thrombocytopenic Purpura | Rigel Pharmaceuticals | October 2014 | Phase 3 |
NCT00706342 | Completed Has Results | Drug: Fostamatinib Disodium / R935788 | Purpura, Thrombocytopenic, Idiopathic | Rigel Pharmaceuticals | January 2007 | Phase 2 |