A potent orally available inhibitor of Syk (Ki = 30 nM); blocks FcεRI-dependent mast cell activation (EC50 = 43 nM) and

R406 – 1 mg

Brand:
Cayman
CAS:
841290-80-0
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

R406 is a potent ATP-competitive inhibitor of spleen tyrosine kinase (Syk, Ki = 30 nM).{25137} Through this action, R406 blocks FcεRI-dependent mast cell activation (EC50 = 43 nM) and, at 3 μM, reduces the release of IL-10, -12, and -13 by immune complex-pulsed dendritic cells.{25137,25138} R406 is orally available and can reduce immune complex-mediated inflammation.{25139} In cancers characterized by over-expression of Syk, R406 can prevent signaling downstream of Syk and induce apoptosis.{25135,20382} R406 also inhibits Syk-dependent signaling through c-Jun N-terminal kinase in rheumatoid arthritis synoviocytes, suggesting a therapeutic intervention in this autoimmune disease.{25136,24052}  

 

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SKU: 11422 - 1 mg Category:

Description

A potent orally available inhibitor of Syk (Ki = 30 nM); blocks FcεRI-dependent mast cell activation (EC50 = 43 nM) and, at 3 μM, reduces the release of IL-10, -12, and -13 by immune complex-pulsed dendritic cells

Formal name: 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one

Synonyms: 

Molecular weight: 470.5

CAS: 841290-80-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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