Fostamatinib disodium (R788, R-935788) is a potent, ATP-competitive and selective Syk (Spleen tyrosine kinase) inhibitor with IC50 of 41 nM. It is an orally available disodium salt of the Syk kinase inhibitor fostamatinib with potential anti-inflammatory and immunomodulating activities. Syk kinase, widely expressed in hematopoietic cells, is a nonreceptor tyrosine kinase that is involved in coupling activated immunoreceptors to signal downstream events that mediate diverse cellular responses, including proliferation, differentiation, and phagocytosis. Fostamatinib disodium (R788) inhibits tumor growth in the Eμ- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. It effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals. The growth-inhibitory effect of Fostamatinib disodium occurs despite the relatively modest cytotoxic effect in vitro and is independent of basal Syk activity, suggesting that Fostamatinib disodium (R788) functions primarily by inhibiting antigen-dependent BCR signals. Importantly, the effect of Fostamatinib disodium was found to be selective for the malignant clones, as no disturbance in the production of normal B lymphocytes was observed.
Molecular Weight | 624.42 |
Formula | C23H24FN6O9PNa2 |
CAS Number | 1025687-58-4 |
Solubility (25°C) | DMSO 18 mg/mL (ultrasonic and warming) |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
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Syk Kinase Peptide Substrate is a Syk kinase peptide substrate. |
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R343
R343 is an immunoglobulin E (IgE) as well as spleen tyrosine kinase (Syk) inhibitor for studies related to allergic asthma and non-small cell lung cancer. |
R333
R333 is a JAK/SYK inhibitor that can be used in studies related to discoid lupus erythematosus (DLE). |
PRT2761
PRT2761 is a spleen tyrosine kinase (Syk) inhibitor that may be used in studies related to allergic conjunctivitis. |
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