枸橼酸托法替尼|T2398|TargetMol

Tofacitinib Citrate
540737-29-9

￥297 5mg 起订

￥496 10mg 起订

￥828 25mg 起订

上海更新日期：2026-01-06

TargetMol中国（陶术生物）

VIP13年

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：: 枸橼酸托法替尼

英文名称：: Tofacitinib Citrate

CAS号：: 540737-29-9

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature,keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

纯度规格：: 99.75%

产品类别：: 抑制剂

货号：: T2398

Product Introduction

Bioactivity

名称	Tofacitinib Citrate
描述	Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
细胞实验	Apoptotic cells were detected by flow cytometry using recombinant human Annexin-V conjugated with allophycocyanin. Briefly, after exposure to CP-690,550 for different periods of time, cells were washed in Ca2+-free PBS and resuspended in 100 μL of binding buffer (10 mM HEPES pH 7.4; 0.15 M NaC1; 5 mM KCl; 1 mM MgCl2; 1.8 mM CaCl2) to which Annexin-V-APC had been previously added. Cells were incubated for 20 min in the dark at room temperature, washed and resuspended in 0.3 mL binding buffer. Cells were analyzed on a FACSCalibur flow cytometer equipped with the Cell Quest Pro software [2].
激酶实验	The JAK1, JAK2, and JAK3 kinase assays utilize a protein expressed in baculovirus-infected SF9 cells (a fusion protein of GST and the catalytic domain of human JAK enzyme) purified by affinity chromatography on glutathione sepharose. The substrate for the reaction was polyglutamic acid-tyrosine [PGT (4:1)], coated onto Nunc Maxi Sorp plates at 100 μg/mL overnight at 37 °C. The plates were washed three times, and JAK enzyme was added to the wells, which contained 100 μL of kinase buffer (50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM sodium orthovanadate). After incubation at room temperature for 30 min, the plates were washed three times. The level of phosphorylated tyrosine in a given well was determined by standard ELISA assay utilizing an anti-phosphotyrosine antibody [5].
动物实验	Mice received tofacitinib in PEG300 (100 mg/ml) or vehicle alone (PEG300) by osmotic pump infusion (Alzet Model 2004, 0.25 μl/hour, 28 days). Four days prior to immunization, mice were anesthetized and their dorsal surface was shaved. A one cm incision was made on the back to create a subcutaneous pocket and insert the pump. The incision site was closed with wound clips. Mice were injected weekly (i.p.) with SS1P recombinant immunotoxin (RIT; 5 μg/mouse) beginning on day 0; control mice received injections of saline alone. Every week before SS1P or vehicle immunization, ~50 μl of blood was drawn to obtain serum samples. Sera were stored at ?80°C until analyzed [4].
体外活性	虽然Tofacitinib (CP-690,550) 对JAK3的抑制作用极为强大（酶抑制效力为1 nM），但其对JAK2和JAK1的抑制作用分别低20至100倍。CP-690,550能以比对GM-CSF诱导的增殖30倍更强的效力抑制IL-2诱导的增殖。CP-690,550在使用鼠、猴或人细胞的混合淋巴细胞反应中展现出强大的抑制效果。与其作用机制一致，这些细胞活性与CP-690,550阻断IL-2诱导的JAK3及其关键底物STAT5的磷酸化能力相关[1]。在治疗含有人类野生型或V617F JAK2的鼠类因子依赖细胞Patersen-erythropoietin receptor (FDCP-EpoR)时，CP-690,550能抑制细胞增殖，其IC50分别为2.1 μg/ml和0.25 μg/ml。对JAK2(V617F)-阳性PV患者体外扩增的红细胞祖细胞进行CP-690,550治疗，表现出特异的抗增殖（IC50：0.2 μg/ml）和促凋亡活性[2]。Tofacitinib对JAK3的药理抑制作用与IMA在CML细胞中的抗肿瘤效果协同增强[3]。
体内活性	CP-690,550治疗显著延长了与对照组相比的移植物存活时间。12只动物中有4只接受CP-690,550治疗（每个剂量组各两只）存活至研究结束，且肾功能正常，根据组织病理学判断只有轻度排斥反应[1]。用tofacitinib单药治疗小鼠能够抑制对由细菌蛋白质Pseudomonas exotoxin A衍生的免疫毒素以及模型抗原钥孔血蓝蛋白的抗体（Ab）反应。实验显示，在免疫后21天观察到对两种抗原IgG1滴度的千倍降低。Tofacitinib治疗还导致CD127+前B细胞数量减少[4]。
存储条件	store at low temperature,keep away from moisture,keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.96 mM), Sonication is recommended. DMSO : 55 mg/mL (109.02 mM), Sonication is recommended.
关键字	Tofacitinib Citrate \| Tofacitinib \| Tasocitinib Citrate \| Tasocitinib \| Janus kinase \| JAK3 \| JAK2 \| JAK1 \| JAK \| Inhibitor \| inhibit \| InfluenzaVirus \| Influenza Virus \| Fungal \| CP-690550 Citrate \| CP690550 Citrate \| CP-690550 \| CP690550 \| CP 690550 Citrate \| CP 690550 \| Bacterial \| Apoptosis
相关产品	Adipic dihydrazide \| Aceglutamide \| Calcium Propionate \| Benzyl propionate \| Levulinic acid \| Neomycin sulfate \| BES \| Terbinafine hydrochloride \| Dimethyl sulfoxide \| Sodium diacetate \| Sulfamethoxazole sodium \| D(+)-Raffinose pentahydrate
相关库	抑制剂库 \| 抗癌上市药物库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗真菌库 \| 激酶抑制剂库 \| 抗病毒库 \| FDA 上市药物库 \| 免疫/炎症分子化合物库 \| 药物功能重定位化合物库 \| FDA 上市激酶抑制剂库 \| 抗癌药物库

柠檬酸托法替尼|||枸橼酸托法替尼|||Tofacitinib (CP-690550) Citrate|||Tasocitinib citrate|||CP-690550 citrate|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	(13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