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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Syk-Fostamatinib
Fostamatinib

Chemical Structure : Fostamatinib

CAS No.: 901119-35-5

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Fostamatinib (R788, R-788)

货号: PC-43349Not For Human Use, Lab Use Only.

Fostamatinib (R788) is a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41 nM.

规格 价格 库存 数量
5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg ￥5280 In stock
250 mg Get quote
1 g Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Fostamatinib (R788) is a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41 nM。
Fostamatinib (R788) dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM, inhibits all phosphorylation events downstream of Syk signaling。
Fostamatinib (R788) specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils. R788 can inhibit local inflammatory injury mediated by immune complexes。
Fostamatinib (R788) reduces immune complex-mediated inflammation in arthritis models.

物理化学性质&存储条件

分子量 580.4595
分子式 C23H26FN6O9P
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one, 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-

参考文献

1. Braselmann S, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

2. Chen L, et al. Blood. 2008 Feb 15;111(4):2230-7.

3. Suljagic M, et al. Blood. 2010 Dec 2;116(23):4894-905.

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