| 应用 |
An inhibitor to spleenic kinase-mediated IgG Fc receptor signaling |
| 产品介绍 |
Fostamatinib (R788)是活性代谢产物R406的前体药物，是一种Syk抑制剂，IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果低5倍。Phase 3。 |
| 备注 |
Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 2. |
| 生化机理 |
R788 (Fostamatinib) is an important spleen tyrosine kinase (Syk) inhibitor, showing efficacy against kinase-mediated IgG Fc gamma receptor signaling. R788 inhibits the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage. In one study, inhibition of BCR signaling with R788 affected the growth of certain leukemia cell lines. These leukemia cells express stereotyped BCRs that react with auto-antigens exposed on the surface of senescent or apoptotic cells, suggesting that they are antigen driven. |
| 别名 |
6-[[5-氟-2-[(3,4,5-三甲氧基苯基)氨基]-4-嘧啶基]氨基]-2,2-二甲基-4-[(磷酰氧基)甲基]-2H-吡啶并[3,2-b]-1,4-恶嗪-3(4H)-酮;R788;(6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2,3-dihydropyrido[3,2-b][1,4]oxazin-4-yl)methyl dihydrogen phosphate;R 788; R-788 |
