Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Tofacitinib 是口服小分子 Janus 激酶抑制剂，用于治疗中度至重度类风湿性关节炎。
| 产品描述 | Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis. |
| 靶点活性 | JAK2:20 nM, JAK1:112 nM, JAK3:1 nM |
| 体外活性 | 每天1.5-15 mg/kg CP-690550长期作用于小鼠,通过流式细胞仪检测,发现淋巴细胞亚群发生剂量和时间依赖性的改变.处理21天,观察到最明显的变化是脾NK1.1+TCRb细胞数降低96%.在用CP-690550（1.87-30 mg/kg,s.c.）处理后,致敏小鼠中的迟发型超敏反应（DTH）反应以剂量依赖性方式降低.CP-690550作用于异位心脏移植(DBA2供体心脏移到C57/BL6宿主)的小鼠模型,导致移植心脏的存活剂量依赖性增加,EC50(50%小鼠将保持移植 >28天时血液中药物浓度)为~60 ng/mL.CP-690550防止非人灵长类动物（NHPs,macaca fascicularis）中同种异体肾脏的排斥(50 到100 ng/ml剂量实验组和200到400 ng/ml剂量实验组的MST分别为62和83天). |
| 体内活性 | CP-690550抑制IL-2诱导的增殖,比对GM-CSF诱导的增殖的效果强30倍。CP-690550高效抑制小鼠混合淋巴反应（MLR）,IC50=91 nM。在小鼠B细胞上CP-690550有效抑制IL-4诱导的CD23上调（IC50 = 57 nM）和II类主要组织相容性复合物（MHCII）表达（IC50 = 71 nM）。CP-690550是特定的口服JAK3抑制剂,作用于JAK2 和 JAK1,效果分别低20和100倍。研究显示低剂量的CP-690550通过加强Th17分化,加速实验性自身免疫脑脊髓炎的发生。 |
| 激酶实验 | JAK3 Kinase Assay: A fragment encoding the catalytic domain of human JAK3 (785aa to 1125aa, JH1 catalytic domain) is amplified by PCR from the full length cDNA and cloned into the EcoRI site of the baculovirus transfer vector pVL1393. Recombinant baculovirus is used to infect Sf9 (Spodoptera frugipedra) cells and recombinant GSTJAK3 fusion protein is isolated on glutathione sepharose. The fusion protein is eluted with reduced glutathione and stored in buffer containing 50 mM Tris, pH 7.5, 10 mM DTT and 10% glycerol. JAK3 kinase activity is measured by ELISA as follows: Plates are coated overnight with a random L-glutamic acid and tyrosine co-polymer (4:1) (100 ug/mL). The plates are washed and recombinant JAK3 JH1:GST (100 ng/well) with or without inhibitors is incubated at room temperature for 30 minutes, after which HRP-conjugated PY20 anti-phosphotyrosine antibody (ICN) is added and developed by TMB (3,3',5,5'-tetramethylbenzidine). Other kinases (Table 1) are produced in E. coli or in insect cells, depending upon what is found to be optimal for the given kinase. The catalytic activity of tyrosine kinases is easured using the aftorementioned ELISA, whereas serine/threonine kinases are assayed using radioactive enzyme assays. |
| 细胞实验 | To measure IL-2-dependent proliferation, isolated lymphocytes are resuspended to a cell density of 1-2 × 106/mL in complete RPMI medium (RPMI 1640 containing 10% (w/v) fetal calf serum (FCS), 1%(w/v) penicillin and treptomycin).Phytohemagluttinin (PHA) is added to a final concentration of 10 mg/mL, and the culture incubated for 3 days at 37 °C in a humidified 5% (v/v) CO2 incubator to upregulate IL-2R and JAK3 expression. IL-2 (200U/mL), with or without CP-690,550 is then added and the cells are incubated for 72 hours at 37 °C in a humidified 5% (v/v) CO2 incubator, after which 50 mL of 3H-thymidine (5mCi/mL) is added. The plates are incubated for an additional 18 hours, harvested with a 96-well harvester, and counted on a scintillation counter. HUO3 cells are maintained in culture with granulocyte-macrophage colony stimulating factor and human foreskin fibroblasts are maintained in culture with 10% fetal calf serum. CP-690550 is added to freshly plated cells and cultured for 4 days. 3Hthymidine is added during the last 18 hours of the culture period. (Only for Reference) |
| 别名 | 托法替尼, Tasocitinib, CP-690550 |
| 分子量 | 312.37 |
| 分子式 | C16H20N6O |
| CAS No. | 477600-75-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
H2O: <1 mg/mL
DMSO: 58 mg/mL (185.7 mM)
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
参考文献文献引用
剂量换算对于不同动物的给药剂量换算，您也可以参考 更多...
体内实验配液计算器请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法： 比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)， 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。
体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300， 混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。
计算器bottom
您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。
Tofacitinib 477600-75-2 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors ROCK JAK Src Janus kinase CP690550 Inhibitor 托法替尼 CP 690550 Tasocitinib inhibit CP-690550 inhibitor
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