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| | R788(Fostamatinib disodium) Basic information |
| Product Name: | R788(Fostamatinib disodium) | | Synonyms: | R788(Fostamatinib disodium);R788, Fostamatinib;R935788 (FostaMatinib disodiuM);FosD;FOSTAMATINIB;FOSD;TAMATINIB FOSDIUM;Tamatinib Fosdium;R788(prodrug of R406);R935788 (FostaMatinib disodiuM, R788) | | CAS: | 1025687-58-4 | | MF: | C23H27FN6NaO9P | | MW: | 604.46 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1025687-58-4.mol |  |
| | R788(Fostamatinib disodium) Chemical Properties |
| Melting point | >191°C (dec.) | | storage temp. | Store at -20°C | | solubility | DMSO (Slightly), Methanol (Slightly) | | form | Solid | | color | Off-White | | Stability: | Hygroscopic |
| | R788(Fostamatinib disodium) Usage And Synthesis |
| Uses | R 788 Sodium Salt is the sodium salt of R 788 which is a selective spleen tyrosine kinase (Syk) inhibitor. It may be used in the treatment of autoimmune diseases such as type 1 diabetes and has been tested in the treatment of rheumatoid athritis, leukemia and lymphoma. | | Biological Activity | r788, which is the prodrug of r406, is a potnet and selective syk inhibitor. the spleen tyrosine kinase (syk) plays a key role in the signaling of activating fc receptors and the b-cell receptor (bcr). | | in vitro | r406 was found to induce the apoptosis of the majority of examined dlbcl cell lines and could specifically inhibit both tonic- and ligand-induced bcr signaling (autophosphorylation of syk525/526 and sykdependent phosphorylation of the b-cell linker protein [blnk]) [1]. | | in vivo | r788 effectively inhibits bcr signaling, demonstrating reduced proliferation and survival of the malignant b cells and significantly prolonged survival of the treated eμ-tcl1 transgenic mouse. moreover, the effect of r788 was found to be selective for the malignant clones, since no disturbance in the production of normal b lymphocytes was observed [2]. | | target | Syk | | references | [1] chen l, monti s, juszczynski p, daley j, chen w, witzig te, habermann tm, kutok jl, shipp ma. syk-dependent tonic b-cell receptor signaling is a rational treatment target in diffuse large b-cell lymphoma. blood. 2008 feb 15;111(4):2230-7.
[2] suljagic m, longo pg, bennardo s, perlas e, leone g, laurenti l, efremov dg. the syk inhibitor fostamatinib disodium (r788) inhibits tumor growth in the eμ- tcl1 transgenic mouse model of cll by blocking antigen-dependent b-cell receptor signaling. blood. 2010 dec 2;116(23):4894-905.
[3] bajpai m. fostamatinib, a syk inhibitor prodrug for the treatment of inflammatory diseases. idrugs. 2009 mar;12(3):174-85. |
| | R788(Fostamatinib disodium) Preparation Products And Raw materials |
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