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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Syk-R788 disodium salt
R788 disodium salt

Chemical Structure : R788 disodium salt

CAS No.: 1025687-58-4

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R788 disodium salt (Fostamatinib disodium salt, R935788)

货号: PC-43348Not For Human Use, Lab Use Only.

Fostamatinib (R788 disodium salt) 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.

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25 mg ￥1980 In stock
50 mg ￥2980 In stock
100 mg ￥4780 In stock
200 mg 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 disodium salt) 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 dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM, inhibits all phosphorylation events downstream of Syk signaling; specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils.
R788 can inhibit local inflammatory injury mediated by immune complexes; reduces immune complex-mediated inflammation in arthritis models.

物理化学性质&存储条件

分子量 624.4232
分子式 C23H24FN6Na2O9P
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]-, sodium salt (1:2)

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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