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Lenvatinib

乐伐替尼,E7080

Lenvatinib (E7080)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。

目录号
EY0870
EY0870
EY0870
EY0870
纯度
99.21%
99.21%
99.21%
99.21%
规格
2 mg
5 mg
10 mg
50 mg
原价
490
810
1100
3960
售价
490
810
1100
3960
库存
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Lenvatinib is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β.

  • 体外研究

  • 体内研究

    0.5% methylcellulose

  • 激酶实验

  • 细胞实验

    0-10 μM

  • 动物实验

    ≤100 mg/kg 口服处理

  • 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] Matsui J, et al. Int J Cancer. 2008, 122(3), 664-671.

    分子式
    C21H19ClN4O4    		 分子量
    426.85    		 CAS号
    417716-92-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    30 mg/mL    		 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
    NCT02640508 Cancer|Solid Tumor Drug: Eribulin|Drug: Lenvatinib Virginia G. Kaklamani|Eisai Inc.|The University of Texas Health Science Center at San Antonio Phase 2 2016-05-01 2016-07-21
    NCT02860936 Adenoid Cystic Carcinomas of the Salivary Glands Drug: Lenvatinib Fondazione IRCCS Istituto Nazionale dei Tumori, Milano Phase 2 2015-06-01 2016-08-04
    NCT02657369 Thyroid Cancer, Anaplastic Drug: Lenvatinib 24 mg Eisai Inc. Phase 2 2016-07-07 2017-02-01
    NCT02199379 Renal Impairment|Disease Severity Drug: Lenvatinib Eisai Inc. Phase 1 2011-11-01 2015-04-13
    NCT02846766 Cancer Drug: Lenvatinib Teresa Helsten, MD|Eisai Co., Ltd.|University of California, San Diego Phase 2 2016-06-01 2016-07-22
    NCT03006926 Hepatocellular Carcinoma Drug: lenvatinib|Drug: pembrolizumab Eisai Co., Ltd.|Eisai Inc. Phase 1 2017-01-01 2016-12-29
    NCT02454478 Carcinoma, Renal Cell Drug: Lenvatinib|Drug: Everolimus Eisai Co., Ltd.|Eisai Inc. Phase 1 2015-07-01 2016-01-19
    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
    NCT03006887 Solid Tumors Drug: lenvatinib|Drug: pembrolizumab Eisai Co., Ltd.|Eisai Inc. Phase 1 2017-01-01 2016-12-29
    NCT01111461 Endometrial Cancer Drug: Lenvatinib Eisai Inc. Phase 2 2010-03-01 2016-11-23
    NCT01321554 Thyroid Cancer Drug: Lenvatinib|Drug: Placebo|Drug: Lenvatinib Eisai Inc. Phase 3 2011-03-01 2017-01-04
    NCT01133977 Stage IV Melanoma Drug: Lenvatinib|Drug: Lenvatinib|Drug: Dacarbazine Eisai Inc.|Quintiles, Inc. Phase 1|Phase 2 2010-04-01 2016-08-16
    NCT02501096 Tumors Drug: Lenvatinib|Drug: Pembrolizumab Eisai Inc. Phase 1|Phase 2 2015-07-22 2017-03-10
    NCT03009292 Solid Tumor Drug: lenvatinib Eisai Inc. Phase 1 2019-01-01 2016-12-31
    NCT02199392 P-glycoprotein|Healthy Volunteers Drug: Lenvatinib Eisai Inc. Phase 1 2011-11-01 2015-02-12
    NCT02702388 Thyroid Cancer Drug: Lenvatinib|Drug: Lenvatinib matching placebo Eisai Inc. Phase 2 2016-03-28 2017-03-13
    NCT02780310 Adenoid Cystic Carcinoma Drug: Lenvatinib Memorial Sloan Kettering Cancer Center|Eisai Inc. Phase 2 2016-05-19 2017-03-02
    NCT01877083 KIF5B-RET-Positive Adenocarcinoma of the Lung Drug: Lenvatinib Eisai Co., Ltd.|Eisai Inc. Phase 2 2013-04-01 2016-09-15
    NCT02686164 Tumors Drug: Lenvatinib|Drug: Midazolam Eisai Inc. Phase 1 2016-05-01 2016-12-13
    NCT02579616 Biliary Tract Cancer Drug: Lenvatinib Eisai Co., Ltd.|Eisai Inc. Phase 2 2015-10-01 2016-11-08
    NCT02953743 Unresectable Hepatocellular Carcinoma (HCC) Drug: Lenvatinib Eisai Co., Ltd.|Eisai Inc. Phase 1 2016-08-01 2016-11-02
    NCT01136967 Unresectable Stage III|Stage IV Melanoma Drug: Lenvatinib Eisai Inc. Phase 2 2010-08-01 2016-02-16
    NCT02578316 Advanced Solid Tumors|Lymphomas Drug: Lenvatinib Eisai Inc. Phase 1 2009-06-01 2015-12-10
    NCT02966093 Differentiated Thyroid Cancer (DTC) Drug: Lenvatinib|Drug: Placebo Eisai Co., Ltd.|Eisai Inc. Phase 3 2017-01-01 2016-11-15
    NCT02792829 Healthy Volunteers Drug: Lenvatinib Eisai Inc. Phase 1 2014-08-01 2016-06-02
    NCT01761266 Hepatocellular Carcinoma (HCC) Drug: Lenvatinib|Drug: Sorafenib Eisai Limited|Eisai Inc. Phase 3 2013-03-01 2017-01-18
    NCT02421042 Hepatic Impairment|Hepatic Function Drug: Lenvatinib Eisai Inc. Phase 1 2011-06-01 2015-05-04
    NCT02562118 Breast Cancer Drug: Lenvatinib + Letrozole National University Hospital, Singapore|Eisai Co., Ltd. Phase 1|Phase 2 2015-09-01 2016-05-29
    NCT01525394 Refractory Solid Tumors|Lymphomas Drug: Lenvatinib|Drug: Moxifloxacin 400 mg|Drug: Placebos (matched to 4 mg and 10 mg lenvatinib capsules). Eisai Inc. Phase 1 2010-12-01 2015-03-03

    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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