Product Information
Kinase Inhibitor Name R788 (Fostamatinib)
FormulaC23H26FN6O9P
SolubilityStability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
CAS No.901119-35-5
Biological ActivityR788 (Fostamatinib) is an important spleen tyrosine kinase (Syk) inhibitor and a free base of R935788 (FosD, fostamatinib disodium, tamatinib fosdium) which is also a selective Syk inhibitor with an IC50 of 41 nM. R788 is an important mediator of immunoreceptor signaling. R788 (Fostamatinib) inhibits Syk kinase-mediated IgG Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage. In a study, R788 (Fostamatinib) was used to treat several types of advanced cancer. In another study, inhibition of BCR signaling with the selective Syk inhibitor R788 (Fostamatinib) will affect the growth of the leukemias that develop in the Eμ-TCL1 transgenic mouse model of CLL. Similarly to human CLL, these leukemias express stereotyped BCRs that react with autoantigens exposed on the surface of senescent or apoptotic cells, suggesting that they are antigen driven. [1][2][3]
M.W.580.46
ReferencesFostamatinib, a Syk-Kinase Inhibitor, Does Not Affect Methotrexate Pharmacokinetics in Patients With Rheumatoid Arthritis Muhammad Baluom, Emil Samara,et al. J Clin Pharmacol 2010;
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 Mirza Suljagic, Pablo G. Longo,et al. Blood 2010;116: 4894-4905
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.