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Lenvatinib (E7080)

Name: Lenvatinib (E7080)
Brand: Selleck Chemicals
SKU: S1164
Rating: 5 (63 reviews)

Catalog No.S1164

For research use only.

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 (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.

CAS No. 417716-92-8

Selleck's Lenvatinib (E7080) has been cited by 63 publications

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VEGFR Signaling Pathway Map

Biological Activity

Description

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)	Click to View More Targets
	4.0 nM	5.2 nM	22 nM	39 nM	Click to View More Targets

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	NXvneZd7TnWwY4Tpc44h[XO\|YYm=	MVq1NQKBkc7:TR?=	NY\PVJZLOjRiaB?=	MkX4WIhmKGmwaHnibZRwenliZX\m[YN1eyCxZjDs[Y53[XSrbnniJI9vKHSqZTD2bYFjcWyrdImgc4Yh[m:2aDDj[YxtKGyrbnXzJJdmemVibn;0JIlv\my3ZX7j[YQh[nlidHjlJIxmeHSrbjD0doVifG2nboSu	NYLOcZN3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5NFY{OjFpPkOwPVA3OzJzPD;hQi=>
ATC cells	MlTXSpVv[3Srb36gZZN{[Xl?	MWWxMEAzPSCjbnSgOVAh\|ryP	NXTaR\|g2PzJiaB?=	NX;McGtWWGixc4Doc5J6dGG2ZXSvco9vNXCqb4PwbI9zgWyjdHXkJGFsfCCxcjDFVmsyNzJicILveIVqdnNiKHX2ZYx2[XSnZDDifUBGVEmVQTmgbY4hdGWwdnH0bY5q[i22cnXheIVlKHOjbYDs[ZMhf2W{ZTDzbYdvcW[rY3HueIx6KHKnZIXj[YQhcW5iQWTDJINmdGxiY4XseJVz\XNw	M4\TbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG3NVA{Lz5{OUWxO\|ExOzxxYU6=
HCC cell lines Hep3B2.1-7, HuH-7, and JHH-7	NV7Nb3llWHKxbHnm[ZJifGmxbjDhd5NigQ>?		MlfCOkBl[Xm\|	NUjuOWZWVGWwdnH0bY5q[iC\|aH;3[YQhe2WuZXP0bZZmKGGwZDDwc5RmdnRiYX70bZBzd2yrZnXyZZRqfmViYXP0bZZqfHliYXfhbY5{fCC2aHWgTGNEKGOnbHygcIlv\XNiSHXwN2IzNjIkgKC3MEBJfUkkgKC3MEBidmRiSljI5qCRPyxid3n0bEBKSzVyII\hcJVmeyCxZjCwMlI{NCByLkSyMEBidmRiMD62OEDPxG2xbD;MMEBz\XOyZXP0bZZmdHlw	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd\|M{WxNUc,Ojl5M{O1NVE9N2F-
HT29 cells	MYnDfZRwfG:6aXPpeJkh[XO\|YYm=	NYS1S3c{OjVuIEWwJI5O	MofUO\|IhcA>?	NWDCTmRz[3m2b4TvfIlkKGSxc3W6JFUxKG6PIHHu[EBvd26leYTveI95cWNiZH;z[VohOjVibl2=	M2fyTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG1OFU3Lz5{NEixOVQ2PjxxYU6=
DX3 and U2OS cells	MWnGeY5kfGmxbjDhd5NigQ>?	Mln3NUDPxE1iYX7kJFExKM7:TR?=	NFf3OoYyPiCqb4Xydy=>	MX3M[Y53[XSrbnniJIlvcGmkaYSgeJVud3JiY3XscJMhdWmpcnH0bY9vKGGwZDDpcpZie2mxbjDheEBkd26lZX70doF1cW:wczD0bIF1KGKxdHigbY5pcWKrdDDpeJMhc26xd36geIFz\2W2czDhcoQh[XKnIHHjbIlmfmGkbHWgZ4xqdmmlYXzsfU4>	NFfacnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe4NVMyPyd-MkG3PFE{OTd:L3G+

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 ; phospho-RET ; Ki-67 / Cyclin D1 / CDK4 / p21 / p53 / Apaf-1 / p-NFκB / Bcl-2 / Cleaved-caspase 3 ; β-catenin ; Vimentin / E-cadherin / Snail / Zeb1	25295214 30286728
Growth inhibition assay	Cell viability	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 (from reference)

Kinase Assay: ^[1]	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]	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.
Animal Research: ^[1]	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.

References

[4] Ana M Molina, et al. Cancer Chemother Pharmacol . 2014 Jan;73(1):181-9.

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Solubility (25°C)

In vitro


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

Chemical Information

Molecular Weight	426.85
Formula	C₂₁H₁₉ClN₄O₄
CAS No.	417716-92-8
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05181033	Not yet recruiting	Drug: Lenvatinib + Letrozole\|Drug: Fulvestrant	Breast Cancer	National University Hospital Singapore\|Eisai Co. Ltd.	January 2022	Phase 2
NCT05171530	Recruiting	Drug: Lenvatinib plus taxane drugs	HER2-negative Advanced Gastric Cancer	Ruijin Hospital	January 5 2022	Phase 1
NCT05112991	Not yet recruiting	Drug: Envafolimab+Lenvatinib\|Drug: Envafolimab	Advanced Endometrial Cancer	3D Medicines (Sichuan) Co. Ltd.\|3D Medicines	January 2022	Phase 2
NCT05081180	Recruiting	Drug: Avelumab\|Drug: Lenvatinib	Central Nervous System Tumors	EMD Serono Research & Development Institute Inc.\|Merck KGaA Darmstadt Germany\|EMD Serono	December 3 2021	Phase 1
NCT05064280	Not yet recruiting	Drug: pembrolizumab\|Drug: Lenvatinib	Brain Metastases\|Tumor	M.D. Anderson Cancer Center\|Eisai Inc.	December 31 2021	Phase 2
NCT05036434	Not yet recruiting	Drug: Pembrolizumab / Lenvatinib	Adrenocortical Carcinoma	National Cancer Center Korea	November 15 2021	Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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