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Tofacitinib Citrate

枸橼酸托法替尼,柠檬酸托法替尼,CP-690550

Tofacitinib (CP-690550) Citrate是一种新型JAK3抑制剂，IC50为1 nM，作用于JAK2和JAK1选择性比其低20到100倍。

目录号
EY0953
EY0953
EY0953
EY0953
EY0953
纯度
99.31%
99.31%
99.31%
99.31%
99.31%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
166
340
580
1420
2300
售价
166
340
580
1420
2300
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Tofacitinib citrate is provided as the citrate salt form of Tofacitinib free base.Tofacitinib (CP-690550) is a potent, selective, and ATP-competitive JAK inhibitor, suppressing all four JAK isoforms with nM potency in in vitro enzyme assays (IC50 values are 3.2 nM, 4.1 nM, 1.6 nM, and 34 nM for JAK1, JAK2, JAK3, and TYK2, respectively), but significantly inhibiting signaling through JAK1 and JAK3 with 5-100 fold selectivity over JAK2 in cellular assays.

  • 体外研究

  • 体内研究

    0.5% methylcellulose

  • 激酶实验

  • 细胞实验

    0.1 μM,1 μM

  • 动物实验

    10, 30 mg/kg/d口服饲喂

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Flanagan ME, et al. J Med Chem, 2010, 53(24), 8468-8484.
    [2] Dowty et al (2013) Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis. J.Pharmacol.Exp.Ther. 348 165.
    [3] Jiang et al (2008) Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J.Med.Chem. 51 8012.

    分子式
    C22H28N6O8    		 分子量
    504.49    		 CAS号
    540737-29-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT03002649 Dermatomyositis Drug: Tofacitinib Johns Hopkins University|Pfizer Phase 1 2017-01-01 2017-01-25
    NCT03011281 Rheumatoid Arthritis Drug: Tofacitinib Hanyang University 2016-11-01 2017-01-04
    NCT02281552 Rheumatoid Arthritis Drug: Tofacitinib|Drug: Tofacitinib Pfizer Phase 3 2014-11-01 2017-01-17
    NCT02299297 Alopecia Areata Drug: Tofacitinib Julian M. Mackay-Wiggan|Locks of Love|Columbia University Phase 2 2015-01-01 2017-02-14
    NCT01202240 Healthy Drug: Tasocitinib (CP-690,55) plus Ketoconazole Pfizer Phase 1 2010-09-01 2011-02-15
    NCT02592434 Juvenile Idiopathic Arthritis Drug: CP-690,550 (tofacitinib)|Other: placebo Pfizer Phase 3 2016-06-10 2017-03-15
    NCT01500551 Juvenile Idiopathic Arthritis Drug: Tofacitinib|Drug: Tofacitinib Pfizer Phase 3 2013-03-18 2017-03-15
    NCT02566967 Rheumatoid Arthritis Drug: tofacitinib Norman B. Gaylis, MD|Arthritis & Rheumatic Disease Specialties Research Phase 3 2015-05-01 2017-01-23
    NCT02812342 Alopecia Areata|Alopecia Totalis|Alopecia Universalis Drug: Tofacitinib ointment Yale University Phase 2 2016-09-01 2016-12-15
    NCT02487433 Healthy Drug: Tofacitinib MR 22 mg (Fed)|Drug: Tofacitinib MR 22 mg (Fasted) Pfizer Phase 1 2015-06-01 2015-08-17
    NCT02084875 Healthy Drug: tofacitinib modified-release (MR) formulation|Drug: tofacitinib modified-release (MR) formulation Pfizer Phase 1 2014-04-01 2014-07-09
    NCT02535689 Systemic Lupus Erythematosus Drug: Tofacitinib|Drug: Placebo National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)|National Institutes of Health Clinical Center (CC) Phase 1 2015-08-25 2017-01-24
    NCT02321930 Rheumatoid Arthritis Drug: tofacitinib 5mg po bid University of California, Los Angeles Phase 4 2016-01-01 2016-08-26
    NCT01976364 Arthritis, Psoriatic Drug: Tofacitinib|Drug: Tofacitinib Pfizer Phase 3 2014-02-17 2017-03-21
    NCT02831855 Rheumatoid Arthritis Drug: CP-690,550|Drug: Methotrexate|Drug: Placebo Pfizer Phase 4 2016-09-01 2017-03-10
    NCT01731327 Healthy Drug: tofacitinib modified-release (MR) formulation|Drug: tofacitinib modified-release (MR) formulation Pfizer Phase 1 2012-11-01 2012-12-20
    NCT02147587 Rheumatoid Arthritis Drug: Tofacitinib|Drug: Placebo Pfizer Phase 2 2014-06-01 2015-07-31
    NCT01164579 Rheumatoid Arthritis Drug: Tasocitinib plus Methotrexate|Drug: Tofacitinib plus placebo methotrexate|Drug: Placebo tofacitinib plus Methotrexate Pfizer Phase 2 2010-10-01 2015-04-21
    NCT01499004 Healthy Drug: tofacitinib (CP-690,550) modified-release formulation A|Drug: tofacitinib (CP-690,550) modified-release formulation B1|Drug: tofacitinib (CP-690,550) modified-release formulation A|Drug: tofacitinib (CP-690,550) modified-release formulation B1|Drug: tofacitinib (CP-690,550) modified-release formulation B2|Drug: tofacitinib (CP-690,550) immediate-release formulation Pfizer Phase 1 2011-11-01 2012-01-11
    NCT02187055 Rhematoid Arthritis Drug: Tofacitinib with methotrexate|Drug: Tofacitinib without methotrexate|Biological: Adalimumab with methotrexate Pfizer Phase 4 2014-08-01 2017-02-14
    NCT03000439 Arthritis Juvenile Idiopathic Drug: In open-label phase: treatment with tofacitinib|Drug: In double-blind phase: treatment with tofacitinib or placebo in 1:1 ratio Pfizer Phase 3 2017-06-16 2017-03-14
    NCT01599377 Healthy Drug: tofacitinib 10 mg|Drug: tofacitinib 5 mg Pfizer Phase 1 2012-05-01 2012-07-08
    NCT01932372 Rheumatoid Arthritis Drug: Tofacitinib (Xeljanz)|Drug: Etanercept, other Biologics, Disease-modifying antirheumatic drugs (DMARDs), etc Pfizer 2013-07-01 2017-03-23
    NCT01226680 Keratoconjunctivitis Sicca Drug: Tasocitinib|Drug: Tasocitinib|Drug: vehicle for Tasocitinib Pfizer Phase 2 2010-12-01 2010-12-21

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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