| Fostamatinib (R788)Spleen tyrosine kinase (Syk) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.15%
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| Cell experiment [1]: | |
Cell lines | Diffuse large B-cell lymphoma (DLBCL) cell lines |
Preparation method | The solubility of this compound in DMSO is > 100.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 4 μM, 96 h |
Applications | R788 was a prodrug of the active metabolite. R406 induced apoptosis of the majority of examined DLBCL cell lines. In R406-sensitive DLBCL cell lines, R406 specifically inhibited both tonic- and ligand-induced BCR signaling (autophosphorylation of SYK525/526 and SYK-dependent phosphorylation of the B-cell linker protein [BLNK]). |
| Animal experiment [2]: | |
Animal models | Eμ- TCL1 transgenic mouse model of CLL, B6/C3H F1 mice |
Dosage form | Intraperitoneal administration, 18 consecutive days at a daily dose of 80 mg/kg |
Application | R788 (80 mg/kg/d) inhibited the growth of adoptively transferred TCL1 leukemias in vivo. R788 treatment administered from days 4 to 25 after adoptive transfer significantly prevented the outgrowth of leukemias. Treatment with R788 significantly prolonged the survival of the animals. In B6/C3H mice, after 4 days of treatment animals receiving R788 showed a greater rise in the number of circulating malignant lymphocytes than controls. In B6/C3H F1 mice, treatment with R788 for 7 days blocked BCR signaling and inhibited leukemic cell survival and proliferation in vivo. In Eμ- TCL1 transgenic mouse model of CLL, R788 inhibited the growth of spontaneously developing TCL1 leukemias. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Chen L, Monti S, Juszczynski P, et al. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma[J]. Blood, 2008, 111(4): 2230-2237. [2]. Suljagic M, Longo P G, Bennardo S, et al. 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[J]. Blood, 2010, 116(23): 4894-4905. | |
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| Cas No. | 901119-35-5 | SDF | Download SDF |
| Chemical Name | [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 dihydrogen phosphate | ||
| 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 | ||
| Formula | C23H26FN6O9P | M.Wt | 580.46 |
| Solubility | ≥100.4mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Fostamatinib is a small molecule inhibitor of spleen tyrosine kinase (Syk) with IC50 value of 41nM [1].
Fostamatinib is an orally bioavailable prodrug of R406. It is developed for the treatment of autoimmune diseases. The effective metabolite of fostamatinib, R406, is an ATP-competitive inhibitor of Syk with Ki value of 30nM. R406 also inhibits the activity of other kinases including Flt3, Lyn (IC50=63nM) and Lck (IC50=37nM). It is found that R406 inhibits both BCR and FcR mediated responses in vitro. Besides that, R406 also shows effects in other cells types and signalling pathways. In the in vivo assay, fostamatinib shows to be highly active to inhibit FcR-mediated signaling in various animal models of allergy, autoimmunity and inflammation. Moreover, fostamatinib also exerts efficacy in SLE animal models. Treatment of fostamatinib suppresses the established renal and skin disease and reduces lymphadenopathy in the MRL/lpr strain [1].
References:[1] McAdoo S P, Tam F W K. Fostamatinib disodium. Drugs of the future, 2011, 36(4): 273.
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缺点也很多。激光的功率很小，对荧光信号的灵敏度和分辨率都很差。只有很强的信号才适合于在这个机器上使用。如果经常要改变染色的步骤，使用不同的样本，或者抗原的量不确定，不建议用这个机器。
比较常用的是用计数微球。比如临床上的CD4细胞绝对计数，就是采用这个方法。试管内事先已经有固定数目的计数微球和染色抗体。按要求加入固定体积的抗凝血液，裂解红细胞后上机。记录一千个微球，同时就会得到不同染色区域细胞的数量。这样就可以算出单位体积血液内CD4细胞的绝对数目了。
这样的计数微球也可以另外购买。浓度是固定的。在你已知体积的细胞悬液中加入一定体积的微球后上机，记录一千个微球的数据，细胞的计数也会同时记录。根据微球的浓度就可以推算出细胞的浓度，从而得出绝对计数了
另外一个方法是有些流式细胞仪是使用微泵加样，而不是连续吸取样本，这样样本的体积是已知的，记录一次就是所有样本的数量，可以算出细胞浓度
正常人T细胞占到淋巴细胞的60-90%。T细胞一般有分为CD4+ 和CD8+这两种，两者的比例正常范围是0.9-6.
2、流式细胞仪（Flow cytometry ）是对细胞进行自动分析和分选的装置。它可以快速测量、存贮、显示悬浮在液体中的分散细胞的一系列重要的生物物理、生物化学方面的特征参量，并可以根据预选的参量范围把指定的细胞亚群从中分选出来。多数流式细胞计是一种零分辨率的仪器，它只能测量一个细胞的诸如总核酸量，总蛋白量等指标，而不能鉴别和测出某一特定部位的核酸或蛋白的多少。也就是说，它的细节 分辨率为零。
我有过两台，一台配有三色激光，当时的报价将近40万美元，最近买的另外一台，两个激光，30万美元。
流失细胞仪检测细胞数量，可能会出现红色的结果吗？
而一些老式 的机器，由于装备的激光数量和检测器都很有限，比如BD calibur这款机器。最高配置也就是蓝色（488nm）和红色（647nm）两种激光。检测4种颜色（通道）。所以为方便起见，就命名为FL1,FL2, FL3和FL4。前三种由于蓝色激光，FL4用于检测红色激光所激发的荧光。其中FL1是检测绿色荧光的（比如FITC，荧光素或者绿色荧光蛋白），而FL2是检测橙色荧光的（比如PI染色）。
染色的各种染料，标记好的荧光抗体染色所需要的缓冲液，封闭液，PBS最终由于上样的缓冲液
