R112

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Chemical Information

Product name：R112	Purity：99% min
CAS NO：575474-82-7	Solubility：DMSO : ≥ 41 mg/mL (131.28 mM)
Molecular Formula：C₁₆H₁₃FN₄O₂	Package：Package according to customer requirements
Molecular Weight：312.298	Storage：Store at -20℃

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Remarks

R112 is a Syk inhibitor. R112 inhibited degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC(50)] = 353 nmol/L) or basophils (histamine release, EC(50) = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC(50) = 490 nmol/L). R112 also blocked leukotriene C4 production and all proinflammatory cytokines tested. Subsequent molecular characterization indicated that R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor (inhibitory constant [K(i)] = 96 nmol/L).

Syk Inhibitors Related Products:

Fostamatinib Disodium; Entospletinib; Fostamatinib

References

[1]. Rossi AB, et al. Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol. 2006 Sep;118(3):749-755.

[2]. Meltzer EO, et al. An intranasal Syk-kinase inhibitor (R112) improves the symptoms of seasonal allergic rhinitis in a park environment. J Allergy Clin Immunol. 2005 Apr;115(4):791-796.