Lenvatinib (E7080)

For research use only.

Catalog No.S1164

31 publications

Lenvatinib (E7080) Chemical Structure

CAS No. 417716-92-8

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 inhibits FGFR1-4, PDGFR, KIT, RET, and shows potent antitumor activities. Phase 3.

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Selleck's Lenvatinib (E7080) has been cited by 31 publications

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Biological Activity

Description 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 inhibits FGFR1-4, PDGFR, KIT, RET, and shows potent antitumor activities. Phase 3.
Targets
RET [4]
()
VEGFR2/KDR [1]
(Cell-free assay)
VEGFR3/FLT4 [1]
(Cell-free assay)
VEGFR1/FLT1 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
4.0 nM 5.2 nM 22 nM 39 nM
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. [1] 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. [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TPC-1 and K1 cells MYDGeY5kfGmxbjDhd5NigQ>? NHnDcG82OOLCid88US=> MkLCNlQhcA>? NY\o[oRIXGinIHnubIljcXSxcomg[YZn\WO2czDv[kBt\W64YYTpcoljKG:wIITo[UB3cWGkaXzpeJkhd2ZiYn;0bEBk\WyuIHzpcoV{KHencnWgco91KGmwZnz1[Y5k\WRiYomgeIhmKGyncITpckB1emWjdH3lcpQv NFTpWpQ{ODlyNkOyNS=>
ATC cells NUfiUHU1TnWwY4Tpc44h[XO|YYm= M1ezW|EtKDJ3IHHu[EA2OCEQvF2= NIS1XHE4OiCq MV\QbI9{eGixconsZZRm\C:wb36tdIhwe3Cqb4L5cIF1\WRiQXv0JI9zKEWUS{GvNkBxem:2ZXnud{Ap\X[jbIXheIVlKGK7IFXMTXNCMSCrbjDs[Y53[XSrbnniMZRz\WG2ZXSgd4FueGynczD3[ZJmKHOrZ37p[olk[W62bImgdoVlfWOnZDDpckBCXENiY3XscEBkfWy2dYLld{4> NIjPb5ozQTVzN{GwNy=>
HCC cell lines Hep3B2.1-7, HuH-7, and JHH-7 M13MWXBzd2yrZnXyZZRqd25iYYPzZZk> M{LhdVYh\GG7cx?= NHm2NoZN\W64YYTpcoljKHOqb4fl[EB{\WynY4TpeoUh[W6mIIDveIVvfCCjboTpdJJwdGmoZYLheIl3\SCjY4Tpeol1gSCjZ3HpcpN1KHSqZTDIR2Mh[2WubDDsbY5meyCKZYCzRlIvOeLCkEesJGh2UOLCkEesJIFv\CCMSFlihLA4NCC5aYToJGlEPTBidnHseYV{KG:oIECuNlMtKDBwNEKsJIFv\CByLk[0JO69dW:uL1ysJJJme3CnY4TpeoVtgS5? NEPEUHAzQTd|M{WxNS=>
HT29 cells M2Llc2N6fG:2b4jpZ4l1gSCjc4PhfS=> MUOyOUwhPTBibl2= MmThO|IhcA>? MoTDZ5l1d3SxeHnjJIRwe2V8IEWwJI5OKGGwZDDuc45kgXSxdH;4bYMh\G:|ZUqgNlUhdk1? NGrYS|QzPDhzNUS1Oi=>
DX3 and U2OS cells Mn3YSpVv[3Srb36gZZN{[Xl? M3\5OFEh|ryPIHHu[EAyOCEQvF2= MWmxOkBpd3W{cx?= Moi5UIVvfmG2aX7pZkBqdmirYnn0JJR2dW:{IHPlcIx{KG2rZ4LheIlwdiCjbnSgbY53[XOrb36gZZQh[2:wY3XueJJifGmxboOgeIhifCCkb4ToJIlvcGmkaYSgbZR{KGuwb4fuJJRiemendIOgZY5lKGG{ZTDhZ4hq\X[jYnzlJINtcW6rY3HscJkv MkDZNlE4QDF|MUe=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
phospho-FGFR1 / FGFR1 /phospho-FRS2 / FRS2 / phospho-MEK / phospho-ERK; 

PubMed: 25295214     


Effect of lenvatinib on FGFR1 signaling pathway in human DTC RO82-W-1 cells in vitro. After starvation overnight, RO82-W-1 cells were treated with vehicle (control), lenvatinib or sorafenib at the indicated concentrations for 1 h and were then stimulated for 10 min with bFGF (20 ng/mL) and heparin before being lysed. Western blot analyses of the phosphorylation of FGFR1 and its downstream effectors in RO82-W-1 cells were then performed and representative images were shown.

phospho-RET; 

PubMed: 25295214     


Western blot analyses of the phosphorylation of RET in human medullary thyroid TT cells. TT cells were seeded and cultured overnight. They were then treated with lenvatinib at the indicated concentrations for 1 h before being lysed.

Ki-67 / Cyclin D1 / CDK4 / p21 / p53 / Apaf-1 / p-NFκB / Bcl-2 / Cleaved-caspase 3; 

PubMed: 30286728     


Immunoblot analysis of cell-cycle arrest and apoptotic proteins in the advanced PTC cell line.

β-catenin; 

PubMed: 30286728     


(a and c) Immunofluorescence assay for nuclear translocation of β-catenin. Results confirmed that SoLAT inhibited nuclear translocation of β-catenin in the advanced PTC cells more potently than either agent alone.

Vimentin / E-cadherin / Snail / Zeb1; 

PubMed: 30286728     


(b and d) Immunoblot analysis of EMT markers showed that most EMT markers such as vimentin, E-cadherin, Snail, and Zeb1 were inhibited by FGFR inhibition (p-ERK1/2) in the SoLAT group.

25295214 30286728
Growth inhibition assay
Cell viability; 

PubMed: 25425971     


Dose-response effects of E7080 on cell viability of human colorectal carcinoma (CRC) cells and endothelial cells (HUVEC). IC50 values were determined in serum reduced (1%) RPMI 1640 medium following treatment with different concentrations of E7080 for 72 hours. The final concentration of DMSO (vehicle) was ≤1%. Results are expressed as the mean ± S.E.M. of at least three independent proliferation assays with hexaplicates.

25425971
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. [1] 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. [2]

Protocol

Kinase Assay:

[1]

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In vitro kinase assay [1]:

Tyrosine kinase assays are performed by HTRF (KDR, VEGFR1, FGFR1, c-Met, EGFR) and ELISA (PDGFRβ), using the recombinant kinase domains of receptors. In both assays, 4 μL of serial dilutions of E7080 are mixed in a 96-well round plate with 10 μL of enzyme, 16 μL of poly (GT) solution (250 ng) and 10 μL of ATP solution (1 μM ATP) (final concentration of DMSO is 0.1%). In wells for blanks, no enzyme is added. In control wells no test article is added. The kinase reaction is initiated by adding ATP solution to each well. After 30-minute incubation at 30°C, the reaction is stopped by adding 0.5 M EDTA (10 μL/well) to the reaction mixture in each well. Dilution buffer adequate to each kinase assay is added to the reaction mixture. In the HTRF assay, 50 μL of the reaction mixture is transferred to a 96-well 1/2 area black EIA/RIA plate, HTRF solution (50 μL/well) is added to the reaction mixture, and then kinase activity is determined by measurement of fluorescence with a time-resolved fluorescence detector at an excitation wavelength of 337 nm and an emission wavelengths of 620 and 665 nm. In the ELISA, 50 μL of the reaction mixture is incubated in avidin coated 96-well polystyrene plates at room temperature for 30 minutes. After washing with wash buffer, PY20-HRP solution (70 μL/well) is added and the reaction mixture is incubated at room temperature for 30 minutes. After washing with wash buffer, TMB reagent (100 μL/well) is added to each well. After several minutes (10–30 minutes), 1 M H3PO4 (100 μL/well) is added to each well. Kinase activity is determined by measurement of absorbance at 450 nm with a microplate reader.
Cell Research:

[2]

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  • Cell lines: HUVECs
  • Concentrations: 0-10 μM
  • Incubation Time: 72 hours
  • Method:

    HUVECs (1,000 cells in each well in serum-free medium containing 2% fetal bovine serum) and L6 rat skeletal muscle myoblasts (5,000 cells in each well in serum-free DMEM) are dispensed in a 96-well plate and incubated overnight. E7080 and either VEGF (20 ng/mL) or FGF-2 (20 ng/mL) containing 2% fetal bovine serum and PDGFβ (40 ng/mL) are added to each well. Cells are incubated for 3 days and then the ratios of surviving cells are measured by WST-1 reagent. For proliferation assay, samples are duplicated and three separate experiments are done.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: H146 tumor cells are implanted subcutaneously (s.c.) into the flank region of female BALB/c nude mice.
  • Dosages: ≤100 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL warmed (93.7 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 426.85
Formula

C21H19ClN4O4

CAS No. 417716-92-8
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl

In vivo Formulation Calculator (Clear solution)

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04519151 Not yet recruiting Drug: Pembrolizumab|Drug: Lenvatinib Ovarian Neoplasms|Carcinoma Ovarian Epithelial|Neoplasm of Stomach|Ovarian Diseases|Genital Neoplasms Female|Ovarian Epithelial Tumor|Urogenital Neoplasms|Neoplasms Glandular and Epithelial Sheba Medical Center November 2020 Phase 2
NCT04447755 Recruiting Drug: Lenvatinib Relapsed or Refractory Solid Tumors Merck Sharp & Dohme Corp.|Eisai Inc. July 30 2020 Phase 2
NCT04287829 Not yet recruiting Drug: Pembrolizumab|Drug: Lenvatinib Mesotheliomas Pleural The Netherlands Cancer Institute|Merck Sharp & Dohme Corp. May 5 2020 Phase 2
NCT04154189 Recruiting Drug: Lenvatinib|Drug: Ifosfamide|Drug: Etoposide Osteosarcoma Eisai Inc. March 25 2020 Phase 2
NCT04042805 Not yet recruiting Biological: Sintilimab|Drug: Lenvatinib Hepatocellular Carcinoma Baocai Xing|Beijing Cancer Hospital August 1 2019 Phase 2
NCT03732495 Recruiting Drug: Lenvatinib + Denosumab Thyroid Cancer Metastatic Centre Leon Berard July 26 2019 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID