R406 (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)

RT

470, 5

Supplied as an off-white powder.

R406 is a potent ATP-competitive inhibitor of spleen tyrosine kinase (Syk, Ki = 30 nM). 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. R406 is orally available and can reduce immune complex-mediated inflammation. In cancers characterized by over-expression of Syk, R406 can prevent signaling downstream of Syk and induce apoptosis. R406 also inhibits Syk-dependent signaling through c-Jun N-terminal kinase in rheumatoid arthritis synoviocytes, suggesting a therapeutic intervention in this autoimmune disease.

Synonyms:
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

CAS No:
841290-80-0

Molecular Formula:
C22H23FN6O5

Molecular Weight:
470.5

Solubility:
DMSO and DMF (0.5mg/ml)

λmax:
220, 278, 336 nm

Appearance:
Crystalline solid

Purity:
≥95%

Storage and Stability:
May be stored at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.