托法替尼|T6321

Tofacitinib
477600-75-2

￥297 5mg 起订

￥483 10mg 起订

￥813 25mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 托法替尼

英文名称：: Tofacitinib

CAS号：: 477600-75-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.71%

产品类别：: 抑制剂

货号：: T6321

Product Introduction

Bioactivity

名称	Tofacitinib
描述	Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3/2/1 (IC50=1/20/112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.
细胞实验	To measure IL-2-dependent proliferation, isolated lymphocytes are resuspended to a cell density of 1-2 × 106/mL in complete RPMI medium (RPMI 1640 containing 10% (w/v) fetal calf serum (FCS), 1%(w/v) penicillin and treptomycin).Phytohemagluttinin (PHA) is added to a final concentration of 10 mg/mL, and the culture incubated for 3 days at 37 °C in a humidified 5% (v/v) CO2 incubator to upregulate IL-2R and JAK3 expression. IL-2 (200U/mL), with or without CP-690,550 is then added and the cells are incubated for 72 hours at 37 °C in a humidified 5% (v/v) CO2 incubator, after which 50 mL of 3H-thymidine (5mCi/mL) is added. The plates are incubated for an additional 18 hours, harvested with a 96-well harvester, and counted on a scintillation counter. HUO3 cells are maintained in culture with granulocyte-macrophage colony stimulating factor and human foreskin fibroblasts are maintained in culture with 10% fetal calf serum. CP-690550 is added to freshly plated cells and cultured for 4 days. 3Hthymidine is added during the last 18 hours of the culture period. (Only for Reference)
激酶实验	JAK3 Kinase Assay: A fragment encoding the catalytic domain of human JAK3 (785aa to 1125aa, JH1 catalytic domain) is amplified by PCR from the full length cDNA and cloned into the EcoRI site of the baculovirus transfer vector pVL1393. Recombinant baculovirus is used to infect Sf9 (Spodoptera frugipedra) cells and recombinant GSTJAK3 fusion protein is isolated on glutathione sepharose. The fusion protein is eluted with reduced glutathione and stored in buffer containing 50 mM Tris, pH 7.5, 10 mM DTT and 10% glycerol. JAK3 kinase activity is measured by ELISA as follows: Plates are coated overnight with a random L-glutamic acid and tyrosine co-polymer (4:1) (100 ug/mL). The plates are washed and recombinant JAK3 JH1:GST (100 ng/well) with or without inhibitors is incubated at room temperature for 30 minutes, after which HRP-conjugated PY20 anti-phosphotyrosine antibody (ICN) is added and developed by TMB (3,3',5,5'-tetramethylbenzidine). Other kinases (Table 1) are produced in E. coli or in insect cells, depending upon what is found to be optimal for the given kinase. The catalytic activity of tyrosine kinases is easured using the aftorementioned ELISA, whereas serine/threonine kinases are assayed using radioactive enzyme assays.
体外活性	方法: 人类 MM 细胞系 MM.1S 与永生化 BMSC 系 HS5 和 HS27A 共培养，用 Tofacitinib (0-10 µM) 处理 24 h，通过 CellTiter-Glo reagent 检测细胞活力。结果: 与单培养生长相比，MM.1S 细胞数量显著增加，证实了该细胞系中基质诱导的增殖信号。Tofacitinib 处理以剂量依赖的方式减少了 MM.1S 细胞数量。Tofacitinib 单独对 MM.1S 细胞存活率或单独对基质细胞没有影响。[1] 方法: NK-92 细胞用 Tofacitinib (50 nM) 处理过夜，再用 IL-15 (2.33 nM) 处理 2 h，检测 STAT1 磷酸化。结果: Tofacitinib 阻断 NK-92 细胞中的 IL-15 信号传导。Tofacitinib 通过阻断 STAT 蛋白磷酸化来破坏 JAK/STAT 信号传导。[2]
体内活性	方法: 为检测体内抗肿瘤活性，用 Tofacitinib (21.5 mg/kg，50% DMSO+10% PEG 400+40% water) 皮下注射给携带原位扩散 MM.1S 异种移植物的 NSG 小鼠，每天一次，持续四周。结果: 小鼠存活率显著提高，并且基于生物发光成像定量，肿瘤负荷显著降低。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 3.12 mg/mL (9.99 mM), Sonication is recommended Ethanol : 0.76 mg/mL (2.43 mM), Sonication is recommended.
关键字	CP 690550 \| Janus kinase \| JAK \| Apoptosis \| Inhibitor \| Tofacitinib \| inhibit \| CP690550
相关产品	L-Glutamic acid \| Metronidazole \| 5-Fluorouracil \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Salicylic acid \| Sodium 4-phenylbutyrate
相关库	经典已知活性库 \| 抗癌上市药物库 \| 已知活性化合物库 \| FDA 上市药物库 \| TGF-β/Smad靶点化合物库 \| 药物功能重定位化合物库 \| FDA 上市激酶抑制剂库 \| 酪氨酸激酶分子库 \| 抗癌临床化合物库 \| 抗癌药物库

托法替尼|||Tasocitinib|||CP-690550|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子