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Ruxolitinib

鲁索利替尼

Ruxolitinib (INCB018424)是选择性的JAK1/2抑制剂，IC50为3.3 nM/2.8 nM。作用于JAK1， JAK2与 作用于JAK3相比，选择性强130倍多。

目录号
EY0699
EY0699
EY0699
EY0699
纯度
99.64%
99.64%
99.64%
99.64%
规格
5 mg
10 mg
25 mg
50 mg
原价
690
995
1800
2600
售价
690
995
1800
2600
库存
现货
现货
现货
现货
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  • 生物活性

    Ruxolitinib dihydrochloride is a specific inhibitor of Janus-associated kinase (JAK1 and JAK2). Ruxolitinib is a small molecular with the formula of C17H21N6O4Pand Molecular Weight of 404. Ruxolitinib phosphate is an administered ATP-competitive cyclopentylpropionitrile derivative and shows inhibition activity on JAK1 and JAK2. Ruxolitinib inhibits phosphorylation of JAK1/2, STAT5, and ERK1/2, resulting in reduced cellular proliferation.

  • 体外研究

  • 体内研究

    5％二甲基乙酰胺，0.5％methocellulose

  • 激酶实验

  • 细胞实验

    3 μM

  • 动物实验

    180 mg/kg 口服

  • 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] Quintas-Cardama A, et al. Blood, 2010, 115(15), 3109-3117.

    分子式
    C17H18N6    		 分子量
    306.37    		 CAS号
    941678-49-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >60 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    15 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
    NCT00638378 Metastatic Prostate Cancer Drug: Ruxolitinib Incyte Corporation Phase 2 2008-02-01 2012-01-20
    NCT01348490 Primary Myelofibrosis|Post Essential Thrombocythemia-myelofibrosis|Post Polycythemia Vera-myelofibrosis Drug: Ruxolitinib (INCB018424) Incyte Corporation Phase 2 2011-06-01 2016-09-23
    NCT01340651 Myelofibrosis Drug: Ruxolitinib Incyte Corporation Phase 2 2011-03-01 2014-02-05
    NCT00726232 Polycythemia Vera|Essential Thrombocythemia Drug: Ruxolitinib Incyte Corporation Phase 2 2008-07-01 2016-10-25
    NCT00674479 Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Myelodysplastic Syndrome|Chronic Myelogenous Leukemia Drug: INCB018424 M.D. Anderson Cancer Center|Incyte Corporation Phase 2 2008-05-01 2016-12-08
    NCT00509899 Myelofibrosis|Polycythemia Vera|Thrombocytosis Drug: Ruxolitinib Incyte Corporation Phase 1|Phase 2 2007-06-01 2016-09-16
    NCT03011892 Atopic Dermatitis Drug: INCB018424 cream|Drug: INCB018424 cream|Drug: INCB018424 cream|Drug: Triamcinolone 0.1% cream|Drug: Vehicle cream Incyte Corporation Phase 2 2016-12-01 2017-01-05
    NCT00639002 Relapsed Multiple Myeloma|Refractory Multiple Myeloma|Multiple Myeloma Drug: Ruxolitinib 25 mg|Drug: Dexamethasone 40 mg Incyte Corporation Phase 2 2008-03-01 2012-06-05
    NCT02553330 Alopecia Areata Drug: Placebo Cream|Drug: INCB018424 Phosphate Cream Incyte Corporation Phase 2 2015-10-01 2016-10-10
    NCT00778700 Plaque Psoriasis Drug: INCB018424 Phosphate Cream|Drug: Placebo Cream Incyte Corporation Phase 2 2008-10-01 2012-03-13
    NCT00952289 Myelofibrosis Drug: Ruxolitinib|Drug: Placebo Incyte Corporation Phase 3 2009-08-01 2016-06-29
    NCT00617994 Plaque Psoriasis Drug: INCB018424 Incyte Corporation Phase 2 2007-08-01 2012-03-13
    NCT01562873 Breast Cancer Drug: Ruxolitinib Dana-Farber Cancer Institute Phase 2 2012-06-01 2017-01-03
    NCT01895842 Leukemia Drug: Ruxolitinib M.D. Anderson Cancer Center|Incyte Corporation Phase 1 2014-02-01 2017-02-06
    NCT00550043 Rheumatoid Arthritis Drug: INCB018424|Drug: Placebo Incyte Corporation Phase 2 2007-10-01 2015-03-09
    NCT03041636 Malignant Neoplasms Stated as Primary Lymphoid Haematopoietic|Other Diseases of Blood and Blood-Forming Organs|Chronic Lymphocytic Leukemia Drug: Ruxolitinib M.D. Anderson Cancer Center|Incyte Corporation Phase 2 2017-03-08 2017-03-09
    NCT01751425 Leukemia Drug: Ruxolitinib|Drug: TKI M.D. Anderson Cancer Center|Incyte Corporation Phase 1|Phase 2 2013-07-01 2016-12-05
    NCT02784496 Myelofibrosis Drug: Ruxolitinib|Behavioral: Questionnaires M.D. Anderson Cancer Center|Incyte Corporation Phase 2 2016-09-01 2016-10-24
    NCT02723994 B-cell Acute Lymphoblastic Leukemia Drug: Ruxolitinib|Drug: Asparaginase Erwinia Chrysanthemi|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Dexamethasone|Drug: Doxorubicin|Drug: Leucovorin Calcium|Drug: Mercaptopurine|Drug: Methotrexate|Drug: Pegaspargase|Drug: Prednisone|Drug: Thioguanine|Drug: Vincristine Sulfate Incyte Corporation|Children's Oncology Group Phase 2 2016-08-01 2017-01-09

    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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