| Identification | Back Directory | [Name]
R788(Fostamatinib disodium) | [CAS]
1025687-58-4 | [Synonyms]
FosD
R 788 sodium
R788 disodium
R 935788 sodium
Tamatinib Fosdium
R788, Fostamatinib
R788 (sodium salt)
FostaMatinib sodiuM
R788(prodrug of R46)
R788 disodium, >=98%
R788(prodrug of R406)
R788; FOSTAMATINIB;R-788
R788(Fostamatinib disodium)
Fostamatinib/R788 disodium)
Fostamatinib Disodium (R788
R788 disodium (Fostamatinib)
R935788 (FostaMatinib disodiuM)
R788; R-935788;R 788 SODIUM;FOSD
FOSTAMATINIB;FOSD;TAMATINIB FOSDIUM
R935788 (FostaMatinib disodiuM, R788)
R788(Fostamatinib disodium) USP/EP/BP
R 788 Sodium Salt
DISCONTINUED. Please see R070115.
Fostamatinib disodium R 788 sodium
Disodium (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2
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
6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one sodium salt
2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one, 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-, sodium salt (1:2)
6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one sodium salt R788 (Fostamatinib) Disodium R 935788 sodium | [Molecular Formula]
C23H24FN6Na2O9P | [MDL Number]
MFCD15146370 | [MOL File]
1025687-58-4.mol | [Molecular Weight]
624.423 |
| Chemical Properties | Back Directory | [Melting point ]
>191°C (dec.) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [color ]
Off-White | [Stability:]
Hygroscopic |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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. |
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