Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
|Solubility (25°C)||DMSO 31.81 mg/mL
Water 2 mg/mL (ultrasonic and warming and heat to 60°C)
|Storage||2-8°C, dry, sealed|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 David J Sweeny, et al. Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation
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ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity.
Dehydroabietinol is an abietane diterpenoid. Dehydroabietinol has kinase inhibition activity for spleen tyrosine kinase (SYK) with an IC50 value of 46.4 μM. Dehydroabietinol can be used for the research of immune-mediated disease.
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