Name: R406
Price: 292.00 USD

- Overview
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    Background
    
    R406 is a potent SYK inhibitorSpleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase mainly expressed in hematopoietic cells. It transmits signals from a variety of cell surface receptors including CD74, Fc receptor and integrins. It is crucial for adaptive immune response, and also very important for cellular adhesion, innate immune recognition, osteoclast maturation, platelet activation and vascular development. [1]
    Functional abnormality of SYK has been implicated in several blood malignancies. Constitutively active SYK can transform B cells. SYK inhibition can be beneficial for patients with blood cancers and autoimmune diseases.
    R406 is a potent inhibitor of IgE and IgG mediated Fc receptor activation with EC50 for degranulation of 56-64 nM. [2] R406 targets SYK and inhibits phosphorylation of SYK substrates by binding to its ATP binding pocket and competing with ATP. R406 strongly inhibits SYK kinase activity with an IC50 of 41 nM.
    R406 induces apoptosis in diffuse large B-cell lymphoma cell lines. It blocks B cell receptor signaling through inhibiton of SYK autophosphorylation of Y525/Y526 and SYK-dependent phosphorylation of the B-cell linker protein. [3]
    R406 can be administrated orally.
    
    [1]Mocsai A, Ruland J, Tybulewicz VL. The SYK tyrosine kinase: a crucial player in diverse biological functions. Nat Rev Immunol 2010. 10(6): 387-402.
    [2]Braselmann S, Taylor V, Zhao H, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther 2006. 319(3): 998-1008.
    [3]Chen L, Monti S, Juszczynski P, et al. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood 2008. 111(4): 2230*2237.
- Properties
  - Alternative Name
    
    benzenesulfonic acid;6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
    
    CAS Number
    
    841290-81-1
    
    Molecular Formula
    
    C22H23FN6O5·C6H6O3S
    
    Molecular Weight
    
    628.63
    
    Appearance
    
    A solid
    
    Purity
    
    98.90%
    
    Solubility
    
    ≥31.45 mg/mL in DMSO; insoluble in H2O; ≥14.95 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Lianghua Xia, Bo Zhang, et al. "Analysis of Syk/PECAM-1 signaling pathway in low shear stress induced atherosclerosis based on ultrasound imaging." Comput Methods Programs Biomed. 2021 Apr;201:105953. PMID:33571923
    2. Xia Wang, Biao Liu, et al. "Blocking podoplanin inhibits platelet activation and decreases cancer-associated venous thrombosis." Thromb Res. 2021 Apr;200:72-80. PMID:33548843
    3. Gao D, Wang L, et al. "Spleen tyrosine kinase SYK(L) interacts with YY1 and coordinately suppresses SNAI2 transcription in lung cancer cells." FEBS J. 2018 Sep 24. PMID:30251328

R406

R406

Background

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