Tofacitinib (CP-690550) Citrate

For research use only. Not for use in humans.

Pfizer辉瑞授权 目录号:S5001 别名: Tasocitinib Citrate 中文名称:托法替尼

Tofacitinib (CP-690550) Citrate Chemical Structure

CAS No. 540737-29-9

Tofacitinib citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂,对JAK3,JAK2,JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1561.36 现货
RMB 1194.19 现货
RMB 2268.63 现货
RMB 3843.17 现货
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客户使用Selleck生产的Tofacitinib (CP-690550) Citrate发表文献159篇:

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 citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂,对JAK3,JAK2,JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。
靶点
JAK3 [1]
(Cell-free assay)
JAK2 [4]
(Cell-free assay)
1 nM 20 nM
体外研究

CP-690550抑制IL-2调节的人T细胞爆发式增殖,和IL-15诱导的CD69表达,IC50分别为11和48 nM。CP-690550抑制混合淋巴细胞反应,IC50为87 nM。CPCP-690550 处理含人野生型或V617F JAK2的鼠因子依赖的细胞Patersen–促红细胞生成素受体(FDCP-EpoR) 细胞,抑制细胞增殖,IC50分别为2.1 µM 和0.25 µM。CP-690550 抑制白细胞介素-6诱导的STAT1 和STAT3磷酸化,IC50分别为23和77 nM。而且, CP-690550作用于携带JAK2V617F的小鼠 FDCP-EpoR细胞,具有显著的促凋亡作用,然而效果比作用于携带野生型JAK2的细胞低。伴随着抑制关键JAK2V617F依赖的下游信号效应器信号转导的磷酸化,及(STAT)3, STAT5, 和v-akt小鼠胸腺瘤病毒癌基因同源(AKT)的转录激活。[2] 此外, CP-690550 在体外作用于人猕猴 NK 和CD8+ T 细胞,抑制IL-15诱导的CD69表达。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
JAK3 / STAT5 / p-STAT5; 

PubMed: 27732937     


The following cell lines: EBV-negative B cell line (BJAB), EBV-transformed lymphoblastoid cell line (LCL), EBV-negative T cell lines (Jurkat and MOLT4), EBV-positive T cell lines (SNT15 and SNT16), EBV-negative NK cell line (KHYG1), and EBV-positive NK cell lines (KAI3 and SNK6), were treated without (−) or with (+) 1 μM tofacitinib for 24 h and cell lysates were then immunoblotted for the indicated proteins.

LMP1 / EBNA1 / BZLF1; 

PubMed: 27732937     


SNT13, SNT15, SNT16, KAI3 and SNK6 cell lines were treated with 5 μM tofacitinib for 48 h, and cell lysates were immunoblotted for LMP1, EBNA1 and BZLF1. Actin was blotted as a loading control.

JAK3 / p-JAK3 / STAT3; 

PubMed: 26082451     


CTCL cell lines were subjected to western blot (tofacitinib 10, 100, 200 nM) (G) after 48 hours of treatment.

27732937 26082451
Growth inhibition assay
Cell number; 

PubMed: 27732937     


BJAB, LCL, Jurkat, SNT15, KHYG1 and KAI3 cells were treated with the indicated concentrations of tofacitinib, and viable cells were counted at the indicated times using the trypan blue exclusion test. Values are means ± SE of the results from triplicate experiments. *P < 0.05 as compared with DMSO-treated cells.

27732937
体内研究 CP-690550 作用于小鼠模型,降低迟发型超敏感反应和延长心脏移植存活。而且, CP-690550 处理来自JAK2V617F阳性 PV患者体内外膨胀的红系祖细胞,产生特定的抗增殖(IC50 = 0.2 µM) 和促凋亡活性。 相反, 在增殖(IC50 > 1.0 µM)和凋亡检测时,从健康对照组中的膨胀祖细胞对CP-690550敏感性低很多。 [2] CP-690550按 10和30 mg/kg剂量每天处理NK细胞,持续处理2周,与对照组相比,细胞数显著降低,这种作用存在时间依赖性。 CP-690550处理实验组的动物效应小样记忆CD8+ 细胞数比对照组低55% 。[3]

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]

- 合并

酶实验:

进行JAK1, JAK2, 和JAK3 激酶实验,使用在杆状病毒感染的 SF9细胞中表达的蛋白(GST 和人类JAK酶催化结构域的融合蛋白),通过亲和层析在谷胱甘肽-琼脂糖凝胶中纯化。反应底物是聚谷氨酸-酪氨酸 [PGT (4:1)], 按100 μg/mL包被到Nunc Maxi Sorp板上,在 37oC下过夜。然后冲洗板三次, 在每孔中加入JAK 酶,孔中含100 μL激酶buffer(50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM 钒酸钠)。按不同剂量加入CP-690550,进行激酶实验。然后在室温下温育30分钟,再冲洗实验板三次。通过标准ELISA实验,使用 磷酸化抗体测定一个给定孔中的磷酸化的酪氨酸水平。
细胞实验:

[2]

- 合并
  • Cell lines: HEL细胞, 扩增的红系祖细胞
  • Concentrations: 0.1 μM,1 μM
  • Incubation Time: 40分钟
  • Method:

    HEL细胞, 从正常供着,两个PV病人体内获得的扩大红系祖细胞,和 FDCP-EpoR受体细胞(每组样本2 × 107 个细胞),使用浓度不断增高的 CP-690550处理, 然后在不同时间点收集。细胞制成颗粒,使用冷磷酸盐缓冲液冲洗三次,然后悬浮在300 µL裂解液中 ,再在冰上处理1小时。细胞裂解液按20 000g转速在 4oC下离心20分钟,取出上清液。在上清液中加入15 µL anti-JAK2 (处理细胞) 或 anti-JAK3 兔抗体(未处理细胞),然后在冰上再处理1小时。最后, 在上清液中加入50 µL 蛋白A/G琼脂糖浆,然后在 4oC下不断旋转温育过夜。冲洗抗体-蛋白复合体三次, 再使用放射免疫沉淀法(RIPA) buffer冲洗一次,使用冲洗冲洗一次,最后使用50 mM Tris-HCl buffer pH 为7.5冲洗一次。通过 Western blotting 分析免疫沉淀复合物,使用磷酸酪氨酸抗体,除去,再使用anti-JAK2和anti-JAK3抗体做探针,来分析免疫沉淀复合物。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: 毛里求斯成年猕猴
  • Dosages: 10, 30 mg/kg/d
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL warmed (198.21 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):
0.5% methylcellulose
30 mg/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 504.49
化学式

C16H20N6O.C6H8O7

CAS号 540737-29-9
储存条件 粉状
溶于溶剂
别名 Tasocitinib Citrate

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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、SDS / 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、SDS / 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04624230 Recruiting Drug: tofacitinib Ulcerative Colitis Pfizer August 12 2021 Phase 3
NCT04496960 Recruiting Drug: tofacitinib|Other: Placebo Sjogren''s Syndrome National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC) May 18 2021 Phase 1|Phase 2
NCT04768504 Not yet recruiting Drug: Tofacitinib 10 mg Immune-Mediated Colitis Khashayar Esfahani|Sir Mortimer B. Davis - Jewish General Hospital April 2021 Phase 2
NCT04424303 Recruiting Drug: Tofacitinib Ulcerative Colitis Pfizer December 7 2020 --
NCT04468425 Recruiting Drug: Tofacitinib Citrate Healthy Subjects TWi Biotechnology Inc. October 14 2020 Phase 1
NCT04338204 Recruiting Drug: tofacitinib Ulcerative Colitis Pfizer September 14 2020 --

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What is the difference between the two products (S5001, S2789)?

  • 回答:

    Tofacitinib (S2789) is the base form of Tofacitinib citrate (S5001). The biological activity of these two compound are same. S5001 is better than S2789 for Oral gavage.

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

相关JAK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID