SML4053
R406
≥98% (HPLC)
别名:
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, N4-(2,2-dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, R 406 (free base), Tamatinib (free base)
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About This Item
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear (Warmed)
儲存溫度
-10 to -25°C
SMILES 字串
CC1(C(NC2=C(O1)C=CC(NC3=NC(NC4=CC(OC)=C(C(OC)=C4)OC)=NC=C3F)=N2)=O)C
生化／生理作用
Orally available, potent, and selective ATP competitive inhibitor of Syk (spleen tyrosine kinase); TAK1 activator.
R406 (Tamatinib) is an orally available, potent, and selective ATP competitive inhibitor of Syk (spleen tyrosine kinase) activity (Ki= 30 nM). R406 potently induces apoptosis in cancer cells overexpressing Syk. R406 is the active metabolite of pro-drug Fostamatinib (R-788). R406 promotes the activation of TAK1 by direct binding to TAK1, independent of its original target Syk kinase.
R406 (Tamatinib) is an orally available, potent, and selective ATP competitive inhibitor of Syk (spleen tyrosine kinase) activity (Ki= 30 nM). R406 potently induces apoptosis in cancer cells overexpressing Syk. R406 is the active metabolite of pro-drug Fostamatinib (R-788). R406 promotes the activation of TAK1 by direct binding to TAK1, independent of its original target Syk kinase.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Attila Mócsai et al.
Nature reviews. Immunology, 10(6), 387-402 (2010-05-15)
Spleen tyrosine kinase (SYK) is known to have a crucial role in adaptive immune receptor signalling. However, recent reports indicate that SYK also mediates other, unexpectedly diverse biological functions, including cellular adhesion, innate immune recognition, osteoclast maturation, platelet activation and
Hoon-Suk Cha et al.
The Journal of pharmacology and experimental therapeutics, 317(2), 571-578 (2006-02-03)
Spleen tyrosine kinase (Syk) is a key regulator of cell signaling induced by cytokines or Fc receptor engagement. However, the role of Syk in rheumatoid arthritis (RA) is not known yet. We investigated the pathways activated by Syk in tumor
Weimin Sun et al.
Proceedings of the National Academy of Sciences of the United States of America, 120(39), e2308079120-e2308079120 (2023-09-21)
TAK1 is a key modulator of both NF-κB signaling and RIPK1. In TNF signaling pathway, activation of TAK1 directly mediates the phosphorylation of IKK complex and RIPK1. In a search for small molecule activators of RIPK1-mediated necroptosis, we found R406/R788
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