Tofacitinib (CP-690550) Citrate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tofacitinib citrate(CP-690550 citrate)是一种有效的JAK3抑制剂。
JAK3是一个造血细胞限制性酪氨酸激酶,参与信号转导,调节淋巴细胞的存活、增殖、分化和凋亡。
Tofacitinib citrate(CP-690550 citrate)对JAK3的抑制是特异性的,比对其它非JAK家族激酶的作用强1000倍。除了抑制JAK3(IC50 = 1 nM),tofacitinib citrate还可以抑制JAK2和JAK1,比对JAK3的作用分别弱20倍和100倍。然而,最近的研究表明,tofacitinib citrate与JAK1、JAK2和JAK3的结合亲和力(Ki)分别是1.6 nM、21.7 nM和6.5 nM。
参考文献:
Lalitha Vijayakrishnan, R. Venkataramanan and Palak Gulati. Treating inflammation with the janus kinase inhibitor CP-690,550. Trends in Pharmacological Sciences 2011: 32 (1); 25-34
- 1. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID:31862381
- 2. McInnes IB, Byers NL, et al. "Comparison of baricitinib, upadacitinib, and tofacitinib mediated regulation of cytokine signaling in human leukocyte subpopulations." Arthritis Res Ther. 2019 Aug 2;21(1):183. PMID:31375130
- 3. Liu S, Verma M, et al. "Steroid resistance of airway type 2 innate lymphoid cells from patients with severe asthma: The role of thymic stromal lymphopoietin."J Allergy Clin Immunol. 2018 Jan;141(1):257-268.e6. PMID:28433687
- 4. Zheng, Lufeng, et al. "The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1." Breast cancer research and treatment (2015): 1-14. PMID:25701119
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 504.49 |
Cas No. | 540737-29-9 |
Formula | C16H20N6O·C6H8O7 |
Synonyms | Tasocitinib citrate,CP 690550 citrate |
Solubility | ≥25.22 mg/mL in DMSO; insoluble in EtOH; ≥3.4 mg/mL in H2O with gentle warming and ultrasonic |
Chemical Name | 2-hydroxypropane-1,2,3-tricarboxylic acid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile |
SDF | Download SDF |
Canonical SMILES | CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
幼稚T细胞 |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
16 h;50 nM |
应用 |
在Th1分化条件下,100 nM和50 nM,而非10 nM的CP-690,550抑制IFN- c的产生。而在Th2分化条件下,10 nM和50 nM的CP-690,550强烈抑制IL-4的产生。这些结果表明,CP-690,550抑制Th1和Th2分化,Th2比Th1对该药物更敏感。进一步检测CP-690,550对Th17和诱导的调节性T(iTreg)细胞的效应。在Th17分化条件下,CP-690,550以剂量依赖的方式增加IL-17的产生,而抑制Foxp3和IL-10的产生。这些数据表明,在体外, |
动物实验[1]: | |
动物模型 |
C57BL6/J小鼠和DBA/1J小鼠 |
剂量 |
30 nM;腹腔注射 |
应用 |
在不同浓度的CP-690,550存在时,从小鼠中分离的幼稚CD4+ T细胞用不同的细胞因子刺激。CP-690,550在3-30 nM时选择性地抑制IFN c诱导的STAT1、IL-4诱导的STAT6和IL-2诱导的STAT5,而30 nM的CP-690,550不能抑制IL-6诱导的STAT3磷酸化。浓度大于100 nM时可部分抑制STAT3。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Yoshida H, Kimura A, Fukaya T, et al. Low dose CP-690,550 (tofacitinib), a pan-JAK inhibitor, accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation[J]. Biochemical and biophysical research communications, 2012, 418(2): 234-240. |
描述 | Tofacitinib (CP-690550)是一个新型的JAK3抑制剂,IC50值为1 nM,比对 JAK2和JAK1的作用分别强20倍和100倍。 | |||||
靶点 | JAK3 | |||||
IC50 | 1 nM |
质量控制和MSDS
- 批次: