Fostamatinib

Fostamatinib Basic information
Product Name:Fostamatinib
Synonyms:Fostamatinib;FostaMatinib DisodiuM;FostaMatinib (R788);R788;NSC-745942;R-935788;R7935788;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
CAS:901119-35-5
MF:C23H26FN6O9P
MW:580.46
EINECS:618-473-2
Product Categories:Inhibitors;API
Mol File:901119-35-5.mol
Fostamatinib Structure
Fostamatinib Chemical Properties
Melting point 214° - 217°C
Boiling point 814.2±75.0 °C(Predicted)
density 1.496
storage temp. -20°C, Hygroscopic
solubility DMSO (Slightly), Methanol (Slightly)
pka1.70±0.10(Predicted)
form Solid
color White to Off-White
Stability:Hygroscopic
Safety Information
MSDS Information
Fostamatinib Usage And Synthesis
UsesFostamatinib can be used to treat cancers that have acquired resistance to kinase inhibitors.
Biological Activityfostamatinib is a small molecule inhibitor of spleen tyrosine kinase (syk) with ic50 value of 41nm [1].fostamatinib is an orally bioavailable prodrug of r406. it is developed for the treatment of autoimmune diseases. the effective metabolite of fostamatinib, r406, is an atp-competitive inhibitor of syk with ki value of 30nm. r406 also inhibits the activity of other kinases including flt3, lyn (ic50=63nm) and lck (ic50=37nm). it is found that r406 inhibits both bcr and fcr mediated responses in vitro. besides that, r406 also shows effects in other cells types and signalling pathways. in the in vivo assay, fostamatinib shows to be highly active to inhibit fcr-mediated signaling in various animal models of allergy, autoimmunity and inflammation. moreover, fostamatinib also exerts efficacy in sle animal models. treatment of fostamatinib suppresses the established renal and skin disease and reduces lymphadenopathy in the mrl/lpr strain [1].
references[1] mcadoo s p, tam f w k. fostamatinib disodium. drugs of the future, 2011, 36(4): 273.
Canertinib Olaparib AZD-9291 Lorlatinib (PF-06463922) Afatinib (BIBW 2992) FostaMatinib DisodiuM Hexahydrate Flavopiridol (Alvocidib) HCl Combretastatin A4 disodium phosphate Brigatinib Dapoxetine Dasatinib AZD 3759 Fosaprepitant dimeglumine Dapoxetine hydrochloride Cabozantinib Selumetinib NU7441 (KU-57788) Poziotinib(HM 781-36B)

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