Lenvatinib (E7080) - Moligand™, 10mM in DMSO , Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor, CAS No.417716-92-8, Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor

CAS: 417716-92-8 Cat. No.: L408456 分子式: C₂₁H₁₉ClN₄O₄ 分子量: 426.85 EC番号: 970-217-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

1-(4-(6-carbamoyl-7-methoxyquinolin-4-yloxy)-2-chlorophenyl)-3-cyclopropylurea

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

Lenvatinib (E7080) is a multi-target inhibitor, mostly forVEGFR2(KDR)/VEGFR3(Flt-4)withIC50of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits
In vitro

E7080, as a potent inhibitor of in vitro angiogenesis, shows a significantly inhibitory effect on VEGF/KDR and SCF/Kit signaling. According to the in vitro receptor tyrosine and serine/threonine kinase assays, E7080 inhibits Flt-1, KDR, Flt-4 with IC50 of 22, 4.0 and 5.2 nM, respectively. In addition to these kinases, E7080 also inhibits FGFR1 and PDGFR tyrosine kinases with IC50 value of 46, 51 and 100 nM for FGFR1, PDGFRα and PDGFRβ, respectively. E7080 potently inhibits phosphorylation of VEGFR2 (IC50, 0.83 nM) and VEGFR3 (IC50, 0.36 nM) in HUVECs which is stimulated by VEGF and VEGF-C, respectively. A recent study shows that E7080 treatment (both at 1 μM and 10 μM) results in a significant inhibition of cell migration and invasion by inhibiting FGFR and PDGFR signaling.

In vivo

When orally administrated in a H146 xenograft model, E7080 inhibits the growth of H146 tumor at 30 and 100 mg/kg in a dose-dependent manner and leads to tumor regression at 100 mg/kg. Furthermore, E7080 at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and imatinib treatment. E7080 significantly inhibits local tumor growth in a MDA-MB-231 mammary fat pad (m.f.p.) model with RTVs (calculated tumor volume on day 8/tumor volume on day 1) of 0.81, and reduces both angiogenesis and lymphangiogenesis of established metastatic nodules of MDA-MB-231 tumor in the lymph nodes.
Cell Data

cell lines：

Concentrations：0-10 μM

Incubation Time：72 hours

Powder Purity:≥98%

Specifications

同義語

1-(4-(6-carbamoyl-7-methoxyquinolin-4-yloxy)-2-chlorophenyl)-3-cyclopropylurea

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

Lenvatinib (E7080) 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 in cell-free assays. Lenvatinib (E7080) also inhi

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

Inhibitor of fms related receptor tyrosine kinase 4;Inhibitor of kinase insert domain receptor

名前と識別子

• 異性体SMILES: COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl
• 代替CAS番号: 417716-92-8
• MeSH用語: 4-(3-chloro-4-(((cyclopropylamino)carbonyl)amino)phenoxy)-7-hydroxy-6-quinolinecarboxamide;4-(3-chloro-4-((cyclopropylaminocarbonyl)amino)phenoxy)-7-methoxy-6-quinolinecarboxamide;4-(3-chloro-4-(N'-cyclopropylureido)phenoxy)-7-methoxyquinoline-6-carboxami
• 分子量: 426.85
• Reaxy-Rn: 12096874
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12096874&ln=

関連ターゲット（人間）

CA5A Tclin Carbonic anhydrase 5A, mitochondrial (1 Activities)

Discover Target: CA5A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (2 Activities)

Discover Target: RET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 (5 Activities)

Discover Target: FLT4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RIPK2 Tchem Receptor-interacting serine/threonine-protein kinase 2 (1 Activities)

Discover Target: RIPK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 (3 Activities)

Discover Target: FLT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (9 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro

参考文献

1. Mengmeng Dong, Yumeng Liu, Yuting Xiao, Qingqing Wu, Mingjing Guan, Zunqiang Xiao, Junwei Liu, Lidong Cao, Yi Lu.  (2025)  Tumor-Targeted PLGA Nanospheres Enhance Therapeutic Effect of Lenvatinib in Hepatocellular Carcinoma via Photothermal and Photodynamic Therapy.  ACS Applied Materials & Interfaces,      [PMID:40689931] [10.1021/acsami.5c09045]

2. Ruoxin Tu, Yining Wang, Ru Xu, Shusheng Wang, Jiabin Cai, Lin Sun, Pengfei Gao.  (2025)  The CCR5/ROS/NRF2 axis Mediates Dihydrotanshinone I-Induced oxidative stress and apoptosis in hepatocellular carcinoma.  BIOCHEMICAL PHARMACOLOGY,      [PMID:40633809] [10.1016/j.bcp.2025.117119]

3. Tongge Li, Shihui Wang, Qianhui Ling, Junyi Sun, Ning Yang, Zhanglei Fu, Zhaoyuan Zhang, Si Chen, Yanfei Wang, Ni Yu, Yafei Wang, Zhexuan Ding, Haodong Liu, Yanwei Jia, Yifang Wang, Xingcai Zhang.  (2025)  Cell Viability, Drug Screening, and Mechanism Study Under Mild Phototherapy Integrated Chemotherapy (PIC).  Advanced Science,      [PMID:40883257] [10.1002/advs.202502836]

4. Huimin Xie, Lin Ma, Xiaoli He, Songsong Zhao, Jin Wang, Ao Zhu, Changming Liu, Olga Piskareva, Chao Deng, Fenghua Meng, Mi Liu.  (2025)  Elevating MHC I expression on tumor cells by nanovesicles loading tyrosine kinase inhibitors can improve the efficacy of cancer vaccines.  Frontiers in Immunology,      [PMID:41019037] [10.3389/fimmu.2025.1653533]

5. Mengming Xia, Xueyi Song, Zebei Lu, Yu Wang, Quan Zhou, Peiwu Geng, Shuanghu Wang, Yunfang Zhou, Qingjun Wu, Aixia Han.  (2023)  Evaluation of the inhibitory effect of azoles on pharmacokinetics of lenvatinib in rats both in vivo and in vitro by UPLC-MS/MS.  Thoracic Cancer,  14  (33): (3331-3341).  [PMID:37771131] [10.1111/1759-7714.15125]

6. Jie Yao, Shuming Tang, Chenyan Shi, Yunzhi Lin, Lanlan Ge, Qinghua Chen, Baoru Ou, Dongyu Liu, Yuyang Miao, Qiujie Xie, Xudong Tang, Jia Fei, Guangyi Yang, Jun Tian, Xiaobin Zeng.  (2022)  Isoginkgetin, a potential CDK6 inhibitor, suppresses SLC2A1/GLUT1 enhancer activity to induce AMPK-ULK1-mediated cytotoxic autophagy in hepatocellular carcinoma.  Autophagy,      [PMID:36048765] [10.1080/15548627.2022.2119353]

7. Dan Wang, Wenqi Ma, Yuanyuan Zhang, Yufeng Wang, Lei Sun, Jue Jiang, Lianying Jiao, Runqing Li, Yujie Zhang, Mingzhen Zhang, Qi Zhou.  (2024)  A versatile nanoplatform carrying cascade Pt nanozymes remodeling tumor microenvironment for amplified sonodynamic/chemo therapy of thyroid cancer.  BIOMATERIALS,      [PMID:39213978] [10.1016/j.biomaterials.2024.122778]

8. Peisen Zheng, Yiqun Xia, Xin Shen, Hui Lu, Yinghua Chen, Chenxin Xu, Chenyu Qiu, Yafei Zhang, Peng Zou, Ri Cui, Xiaoying Huang.  (2024)  Combination of TrxR1 inhibitor and lenvatinib triggers ROS-dependent cell death in human lung cancer cells.  International Journal of Biological Sciences,      [PMID:38164168] [10.7150/ijbs.86160]

9. Yilan Huang, Siwei Wang, Xiaojun Zhang, Chen Yang, Sikai Wang, Hongxia Cheng, Aiwu Ke, Chao Gao, Kun Guo.  (2024)  Identification of Fasudil as a collaborator to promote the anti-tumor effect of lenvatinib in hepatocellular carcinoma by inhibiting GLI2-mediated hedgehog signaling pathway.  PHARMACOLOGICAL RESEARCH,      [PMID:38280440] [10.1016/j.phrs.2024.107082]

10. Jie Yao, Haoqiang Wan, Jingmei Zhang, Wanying Shen, Xiaofang Wei, Chenyan Shi, Baoru Ou, Dongyu Liu, Lanlan Ge, Jia Fei, Xiaobin Zeng.  (2024)  Tubuloside B, a major constituent of Cistanche deserticola, inhibits migration of hepatocellular carcinoma by inhibiting Hippo-YAP pathway.  PHYTOMEDICINE,      [PMID:38552378] [10.1016/j.phymed.2024.155552]

11. Yufeng Deng, Qi hu, Zhiying Song, Mengyuan Nie, Zhiguo Wu, Yongrong Lei, Meng Liu, Dujuan Zhan, Baogang Xie.  (2025)  Mechanism of d-Glucaro-1,4-lactone enhancing the anticancer efficacy of lenvatinib via the IFN-γ-STAT3-PD-L1 signaling pathway in hepatocellular carcinoma.  PHYTOMEDICINE,      [PMID:41485289] [10.1016/j.phymed.2025.157760]

12. Dan Wang, Lei Sun, Juan Wang, Lirong Wang, Zhongyu Wang, Yutong Zhang, Qi Zhou, Yuhang Chen, Jue Jiang.  (2026)  Versatile Nanotherapeutics for Enhancing Sonodynamic/Chemo Therapy of Thyroid Cancer through Remodeling Tumor Microenvironment and Synergistic Reactive Oxygen Species Augment.  Biomaterials Research,      [PMID:41788857] [10.34133/bmr.0338]

13. Wen Luo, Yana Ma, Weijia Zhu, Ruican Nie, Yue Wu, Dongqiu Shan, Shijun Xu, Ho-Young Song, Hongtao Hu.  (2026)  A Biomimetic Mn-Doped Polydopamine Nanoplatform for MRI-Enabled Synergistic Therapy to Enhance Lenvatinib Efficacy in Liver Cancer.  ACS Applied Materials & Interfaces,      [PMID:42003816] [10.1021/acsami.6c00228]

よくある質問

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 417716-92-8, the molecular formula is C21H19ClN4O4, and the molecular weight is 426.85 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.