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Tamibarotene

他米巴罗汀 Am 80

Tamibarotene是RARα激动剂,能诱导HL-60细胞体外分化和凋亡,ED50为0.79 nM。

目录号
EY0812
EY0812
EY0812
EY0812
纯度
99.51%
99.51%
99.51%
99.51%
规格
1 mg
5 mg
10 mg
50 mg
原价
115
230
390
680
售价
115
230
390
680
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Tamibarotene is a synthetic retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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] Sanda T, et al. Leukemia, 2005, 19(6), 901-909.
    [2] The effect of Am-80, a synthetic retinoid, on spinal cord injury-induced motor dysfunction in rats By Takenaga, Mitsuko; Ohta, Yuki; Tokura, Yukie; Hamaguchi, Akemi; Shudo, Koichi; Okano, Hideyuki; Igarashi, Rie From Biological & Pharmaceutical Bulletin (2009), 32(2), 225-231.
    [3] A retinoic acid receptor agonist Am80 rescues neurons, attenuates inflammatory reactions, and improves behavioral recovery after intracerebral hemorrhage in mice By Matsushita, Hideaki; Hijioka, Masanori; Hisatsune, Akinori; Isohama, Yoichiro; Shudo, Koichi; Katsuki, Hiroshi From Journal of Cerebral Blood Flow & Metabolism (2011), 31(1), 222-234.

    分子式
    C22H25NO3
    分子量
    351.44
    CAS号
    94497-51-5
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    70 mg/mL
    Water
    <1 mg/mL
    Ethanol
    70 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
    NCT00520208 Acute Promyelocytic Leukemia Drug: Tamibarotene CytRx Phase 2 2007-09-01 2013-02-11
    NCT01337154 Stage IIIB Non-small Cell Lung Cancer With Pleural Effusion|Stage IV Non-small Cell Lung Cancer Drug: Tamibarotene|Drug: Placebo CytRx Phase 2 2011-04-01 2013-06-27
    NCT00985530 Acute Promyelocytic Leukemia Drug: Tamibarotene|Drug: Arsenic trioxide Northwestern University|CytRx|Cephalon Phase 1 2009-10-01 2013-10-28
    NCT01343355 HTLV-I-Associated Myelopathy Drug: Tamibarotene St. Marianna University School of Medicine Phase 2|Phase 3 2011-01-01 2011-07-21
    NCT01226147 Lupus Nephritis Drug: Tamibarotene Kinki University Phase 2 2010-09-01 2011-07-21
    NCT01120002 Alzheimer's Disease Drug: Tamibarotene|Drug: Placebo Osaka City University Phase 2 2010-05-01 2011-07-21
    NCT00417391 Crohn's Disease Drug: RR110 (Tamibarotene)|Drug: RR110 (Tamibarotene) R&R Inc. Phase 2 2006-12-01 2008-05-25
    NCT02807558 Acute Myeloid Leukemia|Myelodysplastic Syndrome Drug: SY-1425 (tamibarotene)|Drug: azacitidine Syros Pharmaceuticals Phase 2 2016-08-01 2017-03-22

    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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