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Cytarabine

阿糖胞苷

Cytarabine (阿糖胞苷; AraC)具有抗代谢和抗DNA合成活性。

目录号
EY0948
EY0948
纯度
99.11%
99.11%
规格
100 mg
500 mg
原价
475
890
售价
475
890
库存
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Cytarabine (Cytosine arabinoside, AraC) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM. Nucleoside analog of deoxycytidine; inhibits DNA replication by incorporating into DNA (IC50 = 0.04 μM in L1210 and CEM cell lines). Displays no inhibitory effects on RNA synthesis. Causes S phase cell cycle arrest in ML-1 cell lines; cytotoxic in L5817Y leukemia cells. Alternate studies suggest that 1-β-D-Arabinofuranosylcytosine is clastogenic to both spermatogonial cells and bone marrow. Furthermore, 1-β-D-Arabinofuranosylcytosine can be used to control the proliferation of glial cells.

  • 体外研究

  • 体内研究

    Saline

  • 激酶实验

  • 细胞实验

    100 μM 左右

  • 动物实验

    5-1000 mg/kg静脉注射

  • 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 AKm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] Tobias SC, et al. Mol Pharm, 2004, 1(2), 112-116.
    [2] Furth, J.J. and Cohen, S.S. 1968. Cancer Res. 28: 2061-2067.
    [3] Kligerman, A.D., et al. 1999. Mutat. Res. 444: 151-158.
    [4] Palo, A.K., et al. 2009. Mutat. Res. 673: 29-36.

    分子式
    C9H13N3O5
    分子量
    243.22
    CAS号
    147-94-4
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    1 mg/mL
    Water
    50 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
    NCT01191541 Leukemia Drug: Ara-c Chinese Academy of Medical Sciences 2010-05-01 2010-08-30
    NCT00334074 Acute Myelogenous Leukemia|Myelodysplastic Syndromes|Chronic Myelogenous Leukemia Drug: Clofarabine and Cytarabine Baylor Research Institute Phase 2 2005-08-01 2013-07-15
    NCT02652871 Leukemia Drug: LY2510924|Drug: Idarubicin|Drug: Cytarabine M.D. Anderson Cancer Center|Eli Lilly and Company|High Impact Clinical Research Support Program Phase 1 2016-05-01 2017-01-05
    NCT00541866 Acute Myeloid Leukemia Drug: voreloxin injection and cytarabine Sunesis Pharmaceuticals Phase 1|Phase 2 2007-08-01 2012-06-05
    NCT02649764 Leukemia Drug: Fludarabine|Drug: Cytarabine|Drug: LY2606368 M.D. Anderson Cancer Center|Eli Lilly and Company Phase 1 2016-05-01 2017-02-16
    NCT01034410 Acute Myeloid Leukemia Drug: AS1411|Drug: Cytarabine Antisoma Research Phase 2 2010-01-01 2011-02-01
    NCT02718755 Hematologic Malignancy Drug: Fludarabine|Drug: Cytarabine|Drug: Erwinase M.D. Anderson Cancer Center|Jazz Pharmaceuticals Phase 2 2016-12-01 2016-09-19
    NCT01892371 Leukemia Drug: Quizartinib|Drug: Cytarabine|Drug: AZA M.D. Anderson Cancer Center|Ambit Biosciences Corporation|Celgene|National Cancer Institute (NCI) Phase 1|Phase 2 2013-11-01 2017-03-09
    NCT00513305 Acute Myeloid Leukemia Drug: Arsenic trioxide|Drug: Low-dose cytarabine alone Cephalon|Teva Pharmaceutical Industries Phase 3 2007-10-01 2012-07-24
    NCT02926586 Acute Myeloid Leukemia|Core-Binding Factor Drug: Fludarabine|Drug: Cytarabine Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine Phase 4 2016-07-01 2016-10-05
    NCT02840539 Mantle Cell Lymphoma Drug: Bortezomib, Cytarabine, Dexamethasone, Pegteograstim Seoul National University Hospital|Consortium for Improving Survival of Lymphoma Phase 2 2016-10-01 2016-11-01
    NCT00780143 Relapsed/Refractory Leukemia Drug: Plitidepsin plus Cytarabine PharmaMar Phase 1|Phase 2 2007-11-01 2014-10-27
    NCT02930109 Acute Leukemia Drug: PTX-200|Drug: Cytarabine Prescient Therapeutics, Ltd. Phase 1|Phase 2 2016-09-01 2016-10-07
    NCT01615757 Acute Myeloid Leukemia Drug: Ara-c|Drug: Ara-c All India Institute of Medical Sciences, New Delhi Phase 3 2012-08-01 2012-09-13
    NCT01960387 Acute Myeloid Leukemia Drug: Clofarabine|Drug: Cytarabine University of Pittsburgh Phase 2 2013-10-01 2016-06-21
    NCT03021330 AML Drug: Daunomycin and Cytarabine (DA Regimen)|Drug: Daunomycin and Cytarabine (Intermediate Dose of DA Regimen) Institute of Hematology & Blood Diseases Hospital Phase 3 2017-02-08 2017-02-28
    NCT00004263 Leukemia|Myelodysplastic Syndromes Drug: 7-hydroxystaurosporine (UCN-01)|Drug: Cytarabine (Ara-C) M.D. Anderson Cancer Center|National Cancer Institute (NCI) Phase 1 1999-12-01 2012-07-27
    NCT00422591 Leukemia|Acute Myeloid Leukemia|AML Drug: Cytarabine|Drug: Idarubicin M.D. Anderson Cancer Center Phase 2 2006-12-01 2017-01-17
    NCT01656031 Leukemia Drug: clofarabine|Drug: cytarabine Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 2 2005-02-01 2017-02-20
    NCT00516828 Leukemia|Myelodysplastic Syndromes Drug: cytarabine NCIC Clinical Trials Group|Canadian Cancer Trials Group Phase 1|Phase 2 2007-07-01 2015-10-05
    NCT01191801 Leukemia|Acute Myeloid Leukemia|Acute Nonlymphocytic Leukemia Drug: vosaroxin and cytarabine|Drug: placebo and cytarabine Sunesis Pharmaceuticals Phase 3 2010-10-01 2013-10-10
    NCT02670707 Langerhans Cell Histiocytosis Drug: Cytarabine|Drug: Vinblastine/prednisone Baylor College of Medicine|Texas Children's Hospital Phase 3 2016-03-01 2017-01-21

    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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