Fostamatinib (R788)

Fostamatinib (R788)

Catalog Number:
L002370430APE
Mfr. No.:
APE-B2284
Price:
$268
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      • Overview
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          Background

          Fostamatinib 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].

          [1] McAdoo S P, Tam F W K. Fostamatinib disodium. Drugs of the future, 2011, 36(4): 273.

      • Properties
        • Alternative Name
          [6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl dihydrogen phosphate
          CAS Number
          901119-35-5
          Molecular Formula
          C23H26FN6O9P
          Molecular Weight
          580.46
          Purity
          98.00%
          Solubility
          insoluble in H2O; ≥100.4 mg/mL in DMSO; ≥3.05 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

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