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Lenvatinib Mesylate

目录号
EY2208
EY2208
EY2208
EY2208
纯度
99.59%
99.59%
99.59%
99.59%
规格
5 mg
10 mg
25 mg
50 mg
原价
220
365
696
989
售价
220
365
696
989
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    Lenvatinib Mesylate 是一种多靶点抑制剂,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。

  • 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] Takayuki Nakagawa,et al. Lenvatinib in combination with golvatinib overcomes hepatocyte growth factor pathway-induced resistance to vascular endothelial growth factor receptor inhibitor. Cancer Sci. 2014 Jun; 105(6): 723–730. Published online 2014 Apr 28. doi: 10.1111/cas.12409.
    [2] Loredana Lorusso,et al. Lenvatinib and other tyrosine kinase inhibitors for the treatment of radioiodine refractory, advanced, and progressive thyroid cancer. Onco Targets Ther. 2016; 9: 6467–6477. Published online 2016 Oct 20. doi: 10.2147/OTT.S84625.

    分子式
    C21H19ClN4O4.CH4O3S
    分子量
    522.97
    CAS号
    857890-39-2
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    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
    NCT02788708 Fallopian Tube Carcinoma|Recurrent Ovarian Cancer|Primary Peritoneal Carcinoma|Recurrent Endometrial Cancer Drug: Lenvatinib Mesylate|Drug: Paclitaxel|Other: Pharmacological Study Floor Backes|Eisai Inc.|Ohio State University Comprehensive Cancer Center Phase 1 2016-05-27 2017-02-12
    NCT02430714 Thyroid Neoplasms Drug: Lenvatinib Eisai Co., Ltd.|Eisai Inc. 2015-05-20 2017-02-20
    NCT02973997 Columnar Cell Variant Thyroid Gland Papillary Carcinoma|Follicular Variant Thyroid Gland Papillary Carcinoma|Poorly Differentiated Thyroid Gland Carcinoma|Recurrent Thyroid Gland Carcinoma|Stage III Differentiated Thyroid Gland Carcinoma|Stage III Thyroid Gland Follicular Carcinoma|Stage III Thyroid Gland Papillary Carcinoma|Stage IV Thyroid Gland Follicular Carcinoma|Stage IV Thyroid Gland Papillary Carcinoma|Stage IVA Differentiated Thyroid Gland Carcinoma|Stage IVA Thyroid Gland Follicular Carcinoma|Stage IVA Thyroid Gland Papillary Carcinoma|Stage IVB Differentiated Thyroid Gland Carcinoma|Stage IVB Thyroid Gland Follicular Carcinoma|Stage IVB Thyroid Gland Papillary Carcinoma|Stage IVC Differentiated Thyroid Gland Carcinoma|Stage IVC Thyroid Gland Follicular Carcinoma|Stage IVC Thyroid Gland Papillary Carcinoma|Tall Cell Variant Thyroid Gland Papillary Carcinoma|Thyroid Gland Oncocytic Follicular Carcinoma Other: Laboratory Biomarker Analysis|Drug: Lenvatinib|Biological: Pembrolizumab Academic and Community Cancer Research United|National Cancer Institute (NCI) Phase 2 2017-04-01 2017-01-24
    NCT03048877 Differentiated Thyroid Cancer Drug: Apatinib Oral Tablet|Drug: Placebo Oral Tablet Peking Union Medical College Hospital Phase 3 2016-12-01 2017-02-07

    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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