Tofacitinib (CP-690550,Tasocitinib)
(Synonyms: 托法替尼; Tasocitinib; CP-690550) 目录号 : GC16828
Tofacitinib (CP-690550,Tasocitinib) 是一种口服的 JAK3/2/1 抑制剂，IC50 分别为 1、20 和 112 nM。
Cas No.:477600-75-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human T cells and human myelomonocytic cell line HUO3 |
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Preparation method |
The solubility of this compound in DMSO is > 15.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 4000 nM; 4 days |
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Applications |
In human T cell blasts induced by IL-2, CP-690550 inhibited cell proliferation with an IC50 value of 11 nM. In human myelomonocytic HUO3 cells induced by GM-CSF, CP-690550 inhibited cell proliferation with an IC50 value of 324 nM. |
| Animal experiment [1]: | |
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Animal models |
Heterotopic heart transplantation mouse model |
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Dosage form |
0 ~ 136 ng/mL; osmotic minipump infusion |
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Applications |
In a heterotopic heart transplantation mouse model, CP-690550 dose-dependently increased survival of transplanted hearts. Mice received CP-690550 at the concentration of ~ 60 ng/mL maintained their grafts for > 28 days. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH, McCurdy SP, Kudlacz EM, Conklyn MJ, Elliott EA, Koslov ER, Fisher MB, Strelevitz TJ, Yoon K, Whipple DA, Sun J, Munchhof MJ, Doty JL, Casavant JM, Blumenkopf TA, Hines M, Brown MF, Lillie BM, Subramanyam C, Shang-Poa C, Milici AJ, Beckius GE, Moyer JD, Su C, Woodworth TG, Gaweco AS, Beals CR, Littman BH, Fisher DA, Smith JF, Zagouras P, Magna HA, Saltarelli MJ, Johnson KS, Nelms LF, Des Etages SG, Hayes LS, Kawabata TT, Finco-Kent D, Baker DL, Larson M, Si MS, Paniagua R, Higgins J, Holm B, Reitz B, Zhou YJ, Morris RE, O'Shea JJ, Borie DC. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science. 2003 Oct 31;302(5646):875-8. |
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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
[1].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
[2].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.
[3].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.
| Cas No. | 477600-75-2 | SDF | |
| 别名 | 托法替尼; Tasocitinib; CP-690550 | ||
| 化学名 | 3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile | ||
| Canonical SMILES | CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N | ||
| 分子式 | C16H20N6O | 分子量 | 312.37 |
| 溶解度 | ≥ 15.6 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2013 mL | 16.0067 mL | 32.0133 mL |
| 5 mM | 0.6403 mL | 3.2013 mL | 6.4027 mL |
| 10 mM | 0.3201 mL | 1.6007 mL | 3.2013 mL |
| 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 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。