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Fostamatinib Disodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fostamatinib Disodium图片
CAS NO:1025687-58-4
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品名称
Tamatinib Fosdium
R788 disodium
福他替尼二钠盐
R788(Disodium)
R788 (Fostamatinib) Disodium
产品介绍
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)。

产品描述

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

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.

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。

激酶实验

In vitro fluorescence polarization kinase assays: R406 (in vitro active form of R935788) is serially diluted in DMSO and then diluted to 1% DMSO in kinase buffer (20 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM MnCl2, 1 mM DTT, 0.1 mg/mL acetylated BGG). ATP and substrate in kinase buffer are added at room temperature, resulting in a final DMSO concentration on 0.2%. The kinase reactions are performed in a final volume of 20 μL containing 5 μM HS1 peptide substrate and 4 μM ATP and started by addition of 0.125 ng of Syk in kinase buffer. The reaction is allowed to proceed for 40 minutes at room temperature. The reaction is stopped by the addition of 20 μL of PTK quench mix containing EDTA/anti-phosphotyrosine antibody (1× final)/fluorescent phosphopeptide tracer (0.5× final) diluted in FP Dilution Buffer. The plate is incubated for 30 minutes in the dark at room temperature and then read on a Polarion fluorescence polarization plate reader. Data is converted to determine the amount of phosphopeptide present using a calibration curve generated by competition with the phosphopeptide competitor provided in the Tyrosine Kinase Assay Kit. For IC50 determination, R406 is tested at eleven concentrations in duplicate and curve-fitting is performed by non-linear regression analysis using Prism GraphPad Software.

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)

Cas No.

1025687-58-4

分子式

C23H24FN6Na2O9P

分子量

624.43

别名

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

储存和溶解度

Ethanol:<1 mgml
H2O:<1 mgml
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years