Tofacitinib (CP-690550,Tasocitinib)

Pfizer辉瑞授权 目录号:S2789

Tofacitinib (CP-690550,Tasocitinib) Chemical Structure

Molecular Weight(MW): 312.37

Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂,在无细胞试验中IC50为1 nM,作用于JAK2和JAK1选择性低20到100倍。

规格 价格 库存 购买数量  
RMB 744.01 现货
RMB 582.19 现货
RMB 729.41 现货
RMB 2230.13 现货
RMB 3012.77 现货
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客户购买Selleck的此次产品后发表的文献34篇:

客户使用该产品的8个实验数据:

  • (J) Western blotting analysis of HIF1α abundance in response to 100 nM tofacitinib. Quantification of HIF1α detected by Western blot is shown alongside, with data normalized to SMC1 intensity and HIF1α protein abundance in IL-2-maintained cytotoxic T lymphocytes.

    Science, 2018, 11(526), doi: 10.1126/scisignal.aap8112. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

    Effects of CP-690550 on NKTCL cell lines. NK-S1, KHYG-1 cells were treated with CP-690550 for 48 hours, and the effect on STAT5 phosphorylation was evaluated by Western blotting.

    Cancer Discov 2012 2(7), 591-7. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

  • AE cells were treated with vehicle control (DMSO), a MEK inhibitor (PD98059), a PI3K inhibitor (LY294002) or a JAK2 inhibitor (CP690550) at indicated concentrations for 24 hours, followed by lysis for immunoblotting.

    Blood 2012 120(4), 709-19. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

    (d) Immunoblots of indicated proteins in primary EITL cells treated with PD0325901, Tofacitinib and Trametinib for two and Stattic for 24 h at indicated concentrations.

    Leukemia, 2016, 30(6):1311-9. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

  • TRAP-positive multinucleated cell differentiation depends on JAK and is inhibited by tofacitinib in vitro. Effect of tofacitinib on the differentiation of TRAP-positive multi-nucleated cells in vitro (n =3 wells/experiment). Original magnification x 100.

    Arthritis Rheumatol 2014 66(1), 121-9. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

    BMDM from wild time mice were incubated with the concentrations of Ruxolitinib (R) or Tasocitinib (T) indicated, then stimulated for 30 min with (+) or without (-) 500 units/ml IFNβ. The cells were lysed and 30 ug of cell extract protein subjected to SDS-PAGE and immunoblotted with an antibody that recognizes STAT1 phosphorylated at Tyr-701 (p-STAT1) and an antibody that recognizes all forms of STAT1.

    J Biol Chem 2012 287(41), 34825-35. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

  • Effect of a panel of IFN inhibitors on BUNΔNSs virus growth in A549 cells. The inhibitor panel consists of small molecules that target the IKK2 (TPCA-1) and TBK1 (BX795, MRT6884, MRT6707) components of the IFN induction pathway and JAK1 (Cyt387, AZD1480, Ruxolitinib, Tofacitinib) a component of the IFN signaling pathway. Effect of the inhibitors was compared with A549 cells constitutively expressing viral IFN antagonists that block IFN production (BVDV-Npro) or IFN signaling (PIV5-V). Effect of various inhibitor concentrations on plaque size formation. Plaques were visualized 2 days post-infection by crystal violet staining.

    PLoS One 2014 9(11), e112014. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

     

    Role of tyrosine kinase Jak2 in NHE1 activation. Mean (WSEM) pHi increases upon introduction of 350mOsM medium with AG490 (example shown in C), Jak Inhibitor I (Jak Inhibit I; 1uM), CP690550 (1uM), and control (vehicle alone, with 0.1% ethanol for AG490, 0.01% DMSO for Jak Inhibitor I and CP690550). Bars that do not share the same letter are significantly different by one-way ANOVA and Tukey–Kramer Multiple Comparisons Test (P < 0.05).

    Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck.

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂,在无细胞试验中IC50为1 nM,作用于JAK2和JAK1选择性低20到100倍。
靶点
JAK3 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
1 nM 20 nM 112 nM
体外研究

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。CP-690550 对30种其他激酶没有作用效果,平均IC50 > 3000 nM。CP-690,550抑制IL-2诱导的增殖,比作用于GM-CSF诱导的增殖效果强30倍。[1] CP-690550 高效抑制小鼠混合淋巴反应(MLR)(IC50 = 91 nM)。[2] CP-690550 作用于小鼠 B细胞,有效抑制 IL-4 诱导的 CD23 (IC50=57 nM) 和II 类主要组织相容性复合体(MHCII) 表达上调,IC50=71 nM。[3]最新研究显示,通过加强 Th17分化,低剂量CP-690550加速实验性自身免疫脑脊髓炎的发生。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CD4+ T  M1HGVmZ2dmO2aX;uJGF{e2G7 NXzTfGRiOjBxMUCwM|UxOCCwTR?= Mkj3OFghcA>? NFHVXmJqdmirYnn0d{B1cGVibHX2[Yx{KG:oIDDJUE01NCCLRl6t{tMtKEmOLUG3RUBidmRiSVytNlI> NGjjU4czOTh6NEW4NC=>
CD4+ T  MlLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XMU|ExOC93MECgcm0> MUK0PEBp NFu5PYxqdmirYnn0d{BidnSrLVPEN{1qdmS3Y3XkJGNFPCwEoGSgZ4VtdCCycn;sbYZmemG2aX;u NH[0SYczOTh6NEW4NC=>
CD4+ T  MUHGeY5kfGmxbjDBd5NigQ>? NF;IdGYyODBibl2= NXjveVR5OjRxNEigbC=> Ml73ZYJzd2ejdHXzJGNFOy2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUdy=> Mn:2NlE5QDR3OEC=
T cells NVfpO497TnWwY4Tpc44hSXO|YYm= M4\CTlAvOS9yLkOvNUDPxE1? NEPpTmQzPCCq Mn36[Il{enWydIOg{tNkNWOqYXnuJIN6fG:taX7lJJNq\26jbHnu[y=> Mln1NlE{QDN{NEG=

... Click to View More Cell Line Experimental Data

体内研究 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,提高移植后心脏的寿命,这种作用存在剂量依赖性。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 作用于非人灵长类动物 (NHPs, 食蟹猴) (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),防止同种异体肾移植的排斥反应。[1] CP-690550 每天按1.5-15 mg/kg剂量长期作用于小鼠,通过流式细胞仪检测,发现淋巴细胞亚群发生改变,这种作用存在剂量和时间依赖性。处理21天,观察到最显著的变化是脾NK1.1+TCRb 细胞数降低96%。CP-690550 按1.87-30 mg/kg剂量皮下注射给药敏感小鼠,延迟型过敏反应降低,这种作用存在剂量依赖性。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

JAK3 激酶实验:

全长cDNA中编码人JAK3 催化结构域(785aa到 1125aa, JH1 催化结构域)的片段通过PCR放大,且克隆到杆状病毒转移载体 pVL1393的EcoRI位点。使用重组杆状病毒感染 Sf9 细胞,在谷胱甘肽琼脂糖凝胶上分离重组 GSTJAK3融合蛋白。使用还原型谷胱甘肽洗脱融合蛋白,然后储存在含50 mM Tris, pH 7.5, 10 mM DTT 和 10% 甘油的缓冲液中。通过ELISA按如下测量JAK3激酶活性: 使用随机L-谷氨酸和酪氨酸共聚物 (4:1) (100 ug/mL)包被实验板过夜。冲洗实验板,在有或无抑制剂时,重组JAK3 JH1:GST(每孔100 ng)在室温下温育30分钟,然后加入HRP结合的PY20抗磷酸酪氨酸抗体(ICN),然后通过TMB(3,3’,5,5’-四甲基联苯胺)电泳。使用 ELISA法测定酪氨酸激酶催化活性,而通过放射性酶实验测定丝/苏氨酸激酶。
细胞实验:[1]
+ 展开
  • Cell lines: 人类T 细胞
  • Concentrations: 0-4000 nM
  • Incubation Time: 4天
  • Method: 为了测量 IL-2依赖的增殖,分离的淋巴细胞按1-2 × 106/mL密度再悬浮在完全RPMI培养基(RPMI 1640含 10% (w/v)胎牛血清(FCS), 1%(w/v) 青霉素和链霉素 )中。加入植物血细胞凝集素(PHA),终浓度为10mg/mL, 培养物在37oC 下含 5% (v/v) CO2 湿润孵育器中温育3天,用于上调IL-2R 和 JAK3 表达。在有或无CP-690,550 时,加入 IL-2 (200U/mL), 细胞在 37oC下含 5% (v/v) CO2湿润孵育器中温育,72小时后加入50 mL 3H-胸甘(5mCi/mL)。实验板再温育18小时,使用 96孔收集器收集,然后在闪烁计数器中计数。HUO3细胞培养在含粒细胞-巨噬细胞集落刺激因子的培养基中,人包皮成纤维细胞培养在含10% 胎牛血清的培养基中。在新鲜培养的细胞中加入CP-690550,培养4天。在培养期的最后18小时,加入3 H胸甘。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: DBA/2 和 C57/BL6 小鼠
  • Formulation: CP-690550 溶于PEG300
  • Dosages: 0-136 ng/mL
  • Administration: 渗透微泵输入
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 62 mg/mL warmed (198.48 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 312.37
化学式

C16H20N6O

CAS号 477600-75-2
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03502616 Recruiting Ankylosing Spondylitis Pfizer June 7 2018 Phase 3
NCT00413699 Completed Arthritis Rheumatoid Pfizer February 5 2007 Phase 3
NCT03103412 Completed Active Mild Ulcerative Colitis Active Moderate Ulcerative Colitis Healthy Subjects Theravance Biopharma R & D Inc. May 4 2017 Phase 1
NCT03159936 Recruiting Discoid Lupus Erythematosus|Systemic Lupus Erythematosus Tufts Medical Center|Pfizer April 3 2017 Early Phase 1
NCT02535689 Completed Systemic Lupus Erythematosus National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)|National Institutes of Health Clinical Center (CC) August 28 2015 Phase 1
NCT01932372 Active not recruiting Rheumatoid Arthritis Pfizer July 26 2013 --

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操作手册

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常见问题及建议解决方法

  • 问题 1:

    I was just wondering what the main differences between S2789 and S5001?

  • 回答:

    S2789(Tofacitinib (CP-690550)) is the base form of S5001 (Tofacitinib (CP-690550) Citrate). The biological activity of these two compounds are same. The S5001 (Tofacitinib (CP-690550) Citrate) is more suitable for oral administration.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID