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Exemestane

依西美坦,伊西美坦,FCE24304,FCE-24304,FCE 24304,PNU 155971,PNU-155971,PNU155971,

Exemestane是芳香酶(aromatase)抑制剂,能抑制人胎盘和鼠卵巢芳香酶,IC50分别为30 nM和40 nM。

目录号
EY0430
EY0430
EY0430
纯度
99.67%
99.67%
99.67%
规格
1 mg
5 mg
50 mg
原价
110
260
900
售价
110
260
900
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1 μM

  • 动物实验

    100 mg/kg肌肉注射

  • 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] Di Salle E, et al. J Steroid Biochem Mol Biol, 1994, 49(4-6), 289-294.

    分子式
    C20H24O2
    分子量
    296.4
    CAS号
    107868-30-4
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    55 mg/mL
    Water
    <1 mg/mL
    Ethanol
    15 mg/mL

    体内溶解度

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

    NCT00810706 Breast Cancer Drug: exemestane Hellenic Breast Surgeons Society Phase 3 2001-04-01 2008-12-16
    NCT01655004 Breast Carcinoma Drug: Exemestane National University Hospital, Singapore 2012-08-01 2016-06-21
    NCT01965080 Endometrial Cancer Drug: Exemestane Nordic Society for Gynaecologic Oncology Phase 2 2004-03-01 2013-10-15
    NCT01760980 Healthy Drug: Reference product (A) Aromasin (Exemestane)|Drug: Test product (B) Exemestane Actavis Inc. Phase 1 2012-11-01 2014-05-27
    NCT00201773 Breast Cancer Drug: Exemestane|Drug: Celecoxib|Other: Correlative studies Ohio State University Comprehensive Cancer Center|Pfizer Phase 2 2003-07-01 2015-06-25
    NCT01648608 Breast Cancer Drug: Exemestane Tianjin Medical University Phase 2|Phase 3 2012-01-01 2012-08-02
    NCT01743560 Oestrogen Receptor Positive Advanced Breast Cancer Drug: RAD001|Drug: Exemestane Novartis Pharmaceuticals|Novartis Phase 4 2013-01-01 2016-02-24
    NCT00676663 Breast Cancer|Estrogen Receptor-Positive Breast Cancer|Breast Cancer, Estrogen Receptor-Positive|ER+ Breast Cancer Drug: entinostat|Drug: exemestane Syndax Pharmaceuticals Phase 2 2008-05-01 2014-03-19
    NCT00073073 Breast Neoplasms Drug: Exemestane|Dietary Supplement: Calcium carbonate|Dietary Supplement: Vitamin D Georgetown University|National Cancer Institute (NCI) Phase 2 2003-11-01 2016-04-11
    NCT00200174 Breast Cancer Drug: Raloxifene followed by combination therapy|Drug: Exemestane followed by combination therapy Memorial Sloan Kettering Cancer Center|Pharmacia 1999-07-01 2015-12-21
    NCT00919399 Breast Neoplasms Drug: Exemestane|Drug: tamoxifen Institut Claudius Regaud|PHARMACIA SAS Phase 2 2002-01-01 2009-06-11
    NCT01431053 Breast Neoplasms Drug: aspirin|Drug: Exemestane Chinese Academy of Medical Sciences Phase 2 2011-07-01 2013-03-12
    NCT00201864 Breast Cancer Drug: Exemestane|Drug: Fulvestrant Ewa Mrozek|Pfizer|Ohio State University Comprehensive Cancer Center Phase 2 2005-09-01 2016-07-14
    NCT02990845 Premenopausal Breast Cancer Drug: Pembrolizumab/ Exemestane/ Leuprolide National Taiwan University Hospital|Merck Sharp & Dohme Corp. Phase 1|Phase 2 2016-12-01 2016-12-08
    NCT01658176 Breast Neoplasms Drug: PF-04691502|Drug: Exemestane|Drug: Exemestane Pfizer Phase 2 2013-01-01 2012-10-26
    NCT02025712 Hormone Receptor Positive Malignant Neoplasm of Breast Drug: Exemestane|Drug: Everolimus Organisation for Oncology and Translational Research Phase 2 null 2013-12-29
    NCT01155063 Early Breast Cancer Other: Aromasin (exemestane) Pfizer 2010-09-01 2012-09-25
    NCT00031889 Prostate Cancer Drug: Exemestane|Drug: Exemestane+bicalutamide Swiss Group for Clinical Cancer Research Phase 2 2001-08-01 2012-05-14
    NCT00767520 Breast Cancer Drug: Exemestane + Dasatinib|Drug: Exemestane + Placebo Bristol-Myers Squibb Phase 2 2009-02-01 2013-02-22
    NCT00649090 Breast Neoplasms Drug: exemestane Pfizer Phase 4 2005-03-01 2008-09-25

    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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