Tofacitinib 别名：CP-690550, Tasocitinib; 托法替尼
Tofacitinib (CP-690550,Tasocitinib)是一种新型的，具有口服活性的JAK3抑制剂，IC50为1 nM，作用于JAK2和JAK1选择性低20到100倍，可用于炎症性肠病（IBD），斑块状银屑病和斑秃的相关研究。
CAS No.：477600-75-2
Clin Rheumatol. 2025 May 29; .
J Cell Mol Med. 2024 Apr 20;28(7):e18190.
Microglia orchestrate synaptic and neuronal stripping: Implication in neuropsychiatric lupus
Patent. US12138490B2 2024 Nov 12.
Patent. US2023043374A1 2023 Feb 09.
EMBO Mol Med. 2022 Aug 8;14(8):e15653.
Single‐cell transcriptomics reveals a senescence‐associated IL‐6/CCR6 axis driving radiodermatitis
Front Immunol. 2022 May 23;13:866638.
A Novel STAT3 Gain-of-Function Mutation in Fatal Infancy-Onset Interstitial Lung Disease
Front Immunol. 2021 Jul 29;12:675542.
J Virol. 2020 Feb 14;94(5):e01791-19.
Cell Stem Cell. 2019 Apr 4;24(4):654-669.e6.
Patent. US10265258B2 2019 Apr 23.
Arch Dermatol Res. 2018 Oct 5.
Effect of tofacitinib on the expression of noggin/BMP-4 and hair growth stimulation in mice
Patent. JP2018027959A 2018 Feb 22.
Patent. US2018291378A1 2018 Oct 11.
Arch Dermatol Res. 2017 Sep 7.
TJPS. 2017;41 (Supplement Issue): 225-228.
Topical tofacitinib reduce expression of BMP-4 in mouse hair follicle
Patent. JP6212107B2 2017 Oct 11.
Patent. WO2016179605A1 2016 Nov 10.
Sci Adv. 2015 Oct 23.
Pharmacologic inhibition of JAK-STAT signaling promotes hair growth.
Nat Med. 2014 Sep;20(9):1043-9.
Alopecia areata is driven by cytotoxic T lymphocytes and is reversed by JAK inhibition.
化学性质/溶解性/储存
| 分子量 | 312.37 |
| 分子式 | C16H20N6O |
| CAS号 | 477600-75-2 |
| 中文名称 | 托法替尼；托法替尼碱；托法替布 |
| 溶解性 | DMSO ≥60 mg/mL |
| 储存条件 | -20°C, sealed |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
生物活性
实验参考
下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| 浓度/溶剂体积/质量 | 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 |
*吸湿的DMSO对产品的溶解度有显著影响，请使用新开封的DMSO；
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。
| 细胞系 | cytokine-dependent NK92 cell line |
| 方法 | (A) After cytokine starvation for 24 hours, NK92 cells were stimulated by the addition of human IL-2 for 48 hours with and without the addition of serially increasing concentrations of tofacitinib. 3H-thymidine was added during the last 6 hours of the cultures. Cells were then harvested and analyzed for 3H-thymidine incorporation. (B) Cytokine-starved NK92 cells were stimulated with human IL-2, combined IL-6/IL- 6R, or IL-12 for 48 hours with and without serially increasing concentrations of tofacitinib. (C) The NK92 cells were treated as those in panel B with and without a single 50nM dose of tofacitinib. Data are presented as means ±SD (A-C) and are representative of 3 independent experiments. (D) After cytokine starvation for 24 hours, NK92 cells were stimulated with 30 ng/mL of IL-2, 100 ng/mL of combined IL-6/IL-6R, or 100 ng/mL of IL-12 for 1 hour with and without the addition of tofacitinib. The cell lysates were immunoblotted with an anti–phospho-STAT5 monoclonal antibody and an anti-STAT5 antibody. ß-Actin was used as an input control. Data are representative of 3 independent experiments. |
| 浓度 | 0~400 nM |
| 处理时间 | 48 h |
* 上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
建议您制定动物给药及实验方案时，尽量参考已发表的相关实验文献（溶剂种类及配比众多，简单地溶解目的化合物，并不能解决动物给药依从性、体内生物利用度、组织分布等相关问题，未必能保证目的化合物在动物体内充分发挥生物学效用）。
体内实验的工作液，建议您现用现配，当天使用；如在配制过程中出现沉淀、析出现象，可以通过超声和（或）加热的方式助溶。
切勿一次性将产品全部溶解。
请在下面的计算器中，输入您的动物实验相关数据并点击计算，即可得到该实验的总需药量和工作液终浓度。
例如您给药剂量是10 mg/kg，平均每只动物的体重为20 g，每只动物的给药体积是100 μL，动物数量为20只，则该动物实验的总需药量为4 mg，工作液终浓度为2 mg/mL。
1：鉴于实验过程的损耗，建议您至少多配1-2只动物的量；
2：为该产品最终给药时的浓度。
| 动物模型 | IL-15–transgenic CD8 T-cell leukemia–bearing mice |
| 配制 | dissolved in polyethylene glycol 300 (PEG300; VWR Scientific Products) |
| 剂量 | 50 mg/mL |
| 给药处理 | continuously administered via a subcutaneous mini-osmotic pump (ALZET) |
* 上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
其他相关的JAK产品
参考文献
