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Tofacitinib (CP-690550,Tasocitinib)

现货
Catalog No.
A4138
Janus激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
10mg
¥ 500.00
现货
50mg
¥ 970.00
现货

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Background

Tofacitinib, also named CP-690550 orTasocitinib, is a novel oral Janus kinase inhibitor which is being used as a targeted immune-modulator. It primarily inhibits signaling through heterodimeric receptors associated with JAK3, JAK1, or both of them, with functional selectivity over JAK2-paired receptors. Inhibition of JAK1 and JAK3 by tofacitinib blocks signaling for several cytokines, including interleukins 2, 4, 7, 9, 15, and 21. These cytokines are integral to lymphocyte activation, function, and proliferation. Tofacitinib is also an inhibitor of STAT molecules. Recent efforts to investigate the mechanism of action have shown that tofacitinib interacts with multiple JAKs and presumably other kinases

References

Roy Fleischmann, Joel Kremer, John Cush, Hendrik Schulze-Koops, Carol A. Connell, John D. Bradley, David Gruben, Gene V. Wallenstein, Samuel H. Zwillich, and Keith S. Kanik. Placebo-Controlled Trial of Tofacitinib Monotherapy in Rheumatoid Arthritis. N Engl J Med 2012; 367:495-507

William J. Sandborn, Subrata Ghosh, Julian Panes, Ivana Vranic, Chinyu Su, Samantha Rousell, Wojciech Niezychowski. Tofacitinib, an Oral Janus Kinase Inhibitor, in Active Ulcerative Colitis. N Engl J Med 2012; 367:616-624.

Keisuke Maeshima, Kunihiro Yamaoka, Satoshi Kubo, Kazuhisa Nakano, Shigeru Iwata, Kazuyoshi Saito, Masanobu Ohishi, Hisaaki Miyahara, Shinya Tanaka, Koji Ishii, Hironobu Yoshimatsu, Yoshiya Tanaka. The JAK Inhibitor Tofacitinib Regulates Synovitis Through Inhibition of Interferon- and Interleukin-17 Production by Human CD4 T Cells. Arthritis & Rheumatism. 2012. 64(6): 1790–1798.

文献引用

1. Liu S, Verma M, et al. "Steroid Resistance of Airway Type 2 Innate Lymphoid Cells (ILC2s) from Severe Asthma: The Role of Thymic Stromal cell Lymphopoietin (TSLP)." J Allergy Clin Immunol. 2017 Apr 19. pii: S0091-6749(17)30660-7. PMID:28433687

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt312.37
Cas No.477600-75-2
FormulaC16H20N6O
Solubility≥15.6 mg/mL in DMSO, <2.21 mg/mL in EtOH, <2.25 mg/mL in H2O
Chemical Name3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
SDFDownload SDF
Canonical SMILESCC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人T细胞和人骨髓单核细胞系HUO3

制备方法

在DMSO中的溶解度大于15.6 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0 ~ 4000 nM;4天

实验结果

在IL-2诱导的人T细胞中,CP-690550抑制细胞增殖,其IC50值为11 nM。在GM-CSF诱导的人骨髓单核细胞HUO3细胞中,CP-690550抑制细胞增殖,其IC50值为324 nM。

动物实验 [1]:

动物模型

异位心脏移植小鼠模型

给药剂量

0 ~ 136 ng/mL;渗透微泵输液

实验结果

在异位心脏移植小鼠模型中,CP-690550呈剂量依赖性地延长移植心脏的存活时间。给予小鼠~ 60 ng/mL CP-690550,移植器官能存活> 28天。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Changelian PS, Flanagan ME, Ball DJ, et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science. 2003 Oct 31;302(5646):875-8.

质量控制

化学结构

Tofacitinib (CP-690550,Tasocitinib)

相关生物数据

Tofacitinib (CP-690550,Tasocitinib)