Fostamatinib Disodium

CAS号

1025687-58-4

分子式

C23H24FN6O92Na

主要靶点

FLT|Syk

仅限科研使用

Cat No : CM06597

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Synonyms

Inhibitor|inhibit|R788 (Fostamatinib)|R788 (Fostamatinib) Disodium|R788 Disodium|R788(Disodium)|R788|R-788|R 788|Syk|Spleen tyrosine kinase|Tamatinib Fosdium|福他替尼二钠盐|Cluster of differentiation antigen 135|CD135|Fms like tyrosine kinase 3|Fostamatinib|Fostamatinib Disodium|FLT3



产品信息

CAS号 1025687-58-4
分子式 C23H24FN6O92Na
主要靶点 FLT|Syk
主要通路 蛋白酪氨酸激酶|血管生成|血管生成|蛋白酪氨酸激酶
分子量 624.42
纯度 98.95%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|inhibit|R788 (Fostamatinib)|R788 (Fostamatinib) Disodium|R788 Disodium|R788(Disodium)|R788|R-788|R 788|Syk|Spleen tyrosine kinase|Tamatinib Fosdium|福他替尼二钠盐|Cluster of differentiation antigen 135|CD135|Fms like tyrosine kinase 3|Fostamatinib|Fostamatinib Disodium|FLT3

靶点活性

Syk:41 nM

体内活性

在多种弥散性大B细胞淋巴瘤细胞系中(EC50=0.8-8.1 μM),R406降低BLNK, Akt, GSK-3, FOXO和ERK 磷酸化,抑制细胞增殖。

体外活性

在小鼠肿瘤模型中,每天R935788(80 mg/kg)能够有效抑制 TCL1-002, TCL1-551 和 TCL1-870肿瘤生长.在Eμ-TCL1转基因小鼠中,R935788通过阻止抗原依赖性B细胞受体的信号,抑制白血病细胞增殖和存活.

溶解度

Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:50 mg/mL (80.07 mM)

细胞实验

Cells are exposed to increasing concentrations of R406 (in vitro active form of R935788) for 48 hours. The percentage of apoptotic cells is determined by double staining with propidium iodide (PI) and annexin-A5–FITC conjugate. Ki-67 staining is performed with the FITC mouse anti–Ki-67 set. Samples are analyzed on a FACSCalibur flow cytometer with CellQuest Version 3.3 software. (Only for Reference)

参考文献

1.Braselmann S, et al. J Pharmacol Exp Ther, 2006, 319(3), 998-1008.
2.Chen L, et al. Blood, 2008, 111(4), 2230-2237.
3.Suljagic M, et al. Blood, 2010, 116(23), 4894-4905.

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