R788 disodium
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
R788是R406的前体药物，是一种有效的和选择性的Syk抑制剂。Syk（脾酪氨酸激酶）在活化Fc受体和B细胞受体（BCR）的信号传导中起关键作用。
体外实验：R406可以诱导大多数DLBCL细胞系的凋亡，可特异性地抑制紧张和配体诱导的BCR信号，即SYK525/526的自磷酸化以及B细胞接头蛋白[BLNK]的SYK依赖性的磷酸化[1]。
在体实验：R788有效抑制BCR信号，降低恶性B细胞的增殖和存活，使用R788处理Eu-TCL1转基因小鼠，生存时间显著延长。另外，R788对恶性克隆具有选择性，其不影响正常B淋巴细胞的产生[2]。
临床试验：在II期临床试验中，R788治疗有效提高了类风湿关节炎患者的风湿病应答率[3]。
参考文献：
[1] Chen L, Monti S, Juszczynski P, Daley J, Chen W, Witzig TE, Habermann TM, Kutok JL, Shipp MA. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood. 2008 Feb 15;111(4):2230-7.
[2] Suljagic M, Longo PG, Bennardo S, Perlas E, Leone G, Laurenti L, Efremov DG. The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Eμ- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. Blood. 2010 Dec 2;116(23):4894-905.
[3] Bajpai M. Fostamatinib, a Syk inhibitor prodrug for the treatment of inflammatory diseases. IDrugs. 2009 Mar;12(3):174-85.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 624.42 |
| Cas No. | 1025687-58-4 |
| Formula | C23H24FN6Na2O9P |
| Synonyms | Fostamatinib Disodium Hexahydrate;R 788;R-788 |
| Solubility | ≥62.4 mg/mL in DMSO with gentle warming; insoluble in EtOH; ≥2.53 mg/mL in H2O with gentle warming |
| Chemical Name | disodium;[6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl phosphate |
| SDF | Download SDF |
| Canonical SMILES | CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)([O-])[O-])C.[Na+].[Na+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | R788 disodium又被称为Fostamatinib，是活性代谢物的R406的前体药物，是Syk蛋白的抑制剂，IC50为41 nM。 | |||||
| 靶点 | Syk | |||||
| IC50 | 41 nM | |||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
