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Fostamatinib Disodium

Fostamatinib Disodium (R788 Disodium) 是一种口服具有活力的 R406 前药。其中R406 是具有口服活性的，有效的，ATP 竞争性的Syk/FLT3抑制剂(Ki:30 nM，IC50:41 nM)，也能够抑制 Lyn (IC50:63 nM) 和 Lck (IC50:37 nM)。

CAS号

1025687-58-4

分子式

C23H24FN6O9P·2Na

主要靶点

FLT|Syk

仅限科研使用

Cat No : CM06597

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Synonyms

R788(Disodium)|福他替尼二钠盐|R788 Disodium|Tamatinib Fosdium|R788 (Fostamatinib) Disodium

验证数据展示

  • CAS No.: 1025687-58-4

    Fostamatinib Disodium
    CAS#: 1025687-58-4

产品信息

Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulating activities.

CAS号 1025687-58-4
分子式 C23H24FN6O9P·2Na
主要靶点 FLT|Syk
主要通路 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 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 R788(Disodium)|福他替尼二钠盐|R788 Disodium|Tamatinib Fosdium|R788 (Fostamatinib) Disodium

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,H2O:<1 mg/mL,DMSO:10 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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