Lenvatinib (E7080; ER-203492-00)

Alias: E-7080; E7080; E 7080; ER-203492-00; Lenvatinib; Brand name: Lenvima
Cat No.:V0508 Purity: ≥98%
Lenvatinib (formerly E-7080, ER-203492-00; tradename Lenvima among others) is a potent and orally bioavailablemulti-targeted kinase [VEGFR2(KDR)/VEGFR3(Flt-4)]inhibitorwith potential antitumor activity.
Lenvatinib (E7080; ER-203492-00) Chemical Structure CAS No.: 417716-92-8
Product category: VEGFR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
2mg
5mg
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1g
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Other Forms of Lenvatinib (E7080; ER-203492-00):

  • Lenvatinib mesylate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Lenvatinib (formerly E-7080, ER-203492-00; trade name Lenvima among others) is a potent and orally bioavailable multi-targeted kinase [VEGFR2(KDR)/VEGFR3(Flt-4)] inhibitor with potential antitumor activity. With IC50 values of 4 nM and 5.2 nM, respectively, it inhibits VEGFR2/VEGFR3, and in cell-free assays, it has less potency against VEGFR1/Flt-1. In 2015, lenitinib was licensed for the treatment of differentiated thyroid cancer that was not responsive to radioactive iodine (radioiodine) treatment and was either locally recurrent or metastatic.

Biological Activity I Assay Protocols (From Reference)
Targets
VEGFR1 (IC50 = 22 nM); VEGFR2 (IC50 = 4 nM); VEGFR3 (IC50 = 5.2 nM); FGFR1 (IC50 = 46 nM); PDGFRα (IC50 = 51 nM); PDGFRβ (IC50 = 39 nM); c-Kit (IC50 = 100 nM); FGFR2; FGFR3; FGFR4; RET
ln Vitro
Lenvatinib (E7080) has IC50s of 4, 5.2, and 22 nM for VEGFR1 (Flt-1), VEGFR3 (Flt-4), and VEGFR2 (KDR), in that order. FGFR1, PDGFRβ, KIT, and TCGF are all inhibited by lentinib, with IC50 values of 51, 39, 46, and 100 nM, respectively[3].
ln Vivo
Lenvatinib (E7080) (100 mg/kg, p.o.) also significantly inhibits metastasis to both distant lung and regional lymph nodes after treatment concludes, in addition to significantly inhibiting local tumor growth at the m.f.p.[3]. Lenvatinib (E7080) causes tumor regression in the H146 xenograft model at 100 mg/kg and dose-dependently suppresses the growth of the H146 tumor at 30 and 100 mg/kg (BID, QDx21). Lenvatinib at 100 mg/kg reduces microvessel density more than anti-VEGF antibody and STI571 treatment, according to IHC analysis using anti-CD31 antibody[4].
Enzyme Assay
Recombinant kinase domains of receptors are used in HTRF (KDR, VEGFR1, FGFR1, c-Met, EGFR) and ELISA (PDGFRβ) tyrosine kinase assays. In both assays, 10 μL of enzyme, 16 μL of poly (GT) solution (250 ng), and 10 μL of ATP solution (1 μM ATP) are combined with 4 μL of serial dilutions of E7080 in a 96-well round plate (final concentration of DMSO is 0.1%). Enzyme is not added to blank wells. There is no test article added to control wells. Each well receives an addition of ATP solution to start the kinase reaction. The reaction is terminated by adding 0.5 M EDTA (10 μL/well) to the reaction mixture in each well following a 30-minute incubation period at 30°C. The reaction mixture is supplemented with dilution buffer appropriate for each kinase assay. The HTRF assay involves transferring 50 μL of the reaction mixture to a 96-well 1/2 area black EIA/RIA plate, adding 50 μL of HTRF solution per well, and measuring the fluorescence of the reaction mixture using a time-resolved fluorescence detector at 620 and 665 nm for emission and 337 nm for excitation. This allows for the determination of kinase activity. For the ELISA, 96-well polystyrene plates coated with avidin are incubated at room temperature for 30 minutes with 50 μL of the reaction mixture. Following washing with wash buffer, the reaction mixture is incubated at room temperature for 30 minutes before PY20-HRP solution (70 μL/well) is added. In each well, 100 μL of TMB reagent is added following washing with wash buffer. Each well receives 100 μL of 1 M H3PO4 after a few minutes (10–30 minutes). By measuring absorbance at 450 nm with a microplate reader, kinase activity can be identified.
Cell Assay
H146 (1.2×103 cells/50 μL/well) are cultured in 96-well multi-plates with SFM containing 0.5% BSA. Following an overnight culture at 37°C, SFM (150 μL/well) containing 0.5% FBS and various SCF concentrations are added, either with or without various compound concentrations. WST-1 is used to measure the ratios of surviving cells following a 72-hour culture.
Animal Protocol
Clean-room conditions are used to maintain 8–12 week old, 20–25 g female BALB/c nude mice. Mice's flanks are subcutaneously (s.c.) implanted with 6.5×106 H146 tumor cells. Day 1 of the experiment occurs twelve days after the injection when mice are randomized into treatment (n = 6 or n = 5) and control (n = 12) groups. From day one to day twenty-one, lenvatinib, STI571, and VEGF neutralization antibody are given orally twice daily for lenvatinib and STI571 and twice weekly for the antibody. These substances are suspended in 0.5% methylcellulose and saline, respectively. On the designated days, tumor volume is measured and computed. Relative tumor volume (RTV) is a measure of antitumor activity that is calculated as the volume of the tumor on day 1 divided by the tumor volume at indicated days.
References

[1]. Lenvatinib versus Bay 43-9006 in first-line treatment of patients with unresectable hepatocellularcarcinoma: a randomised phase 3 non-inferiority trial. Lancet. 2018 Mar 24;391(10126):1163-1173.

[2]. Lenvatinib: A Promising Molecular Targeted Agent for Multiple Cancers. Cancer Control. 2018 Jan-Dec;25(1):1073274818789361.

[3]. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008, 122(3), 664-671.

[4]. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase. Clin Cancer Res. 2008, 14(17),545.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H19CLN4O4
Molecular Weight
426.85
Exact Mass
426.11
Elemental Analysis
C, 59.09; H, 4.49; Cl, 8.30; N, 13.13; O, 14.99
CAS #
417716-92-8
Appearance
Solid powder
SMILES
COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl
InChi Key
WOSKHXYHFSIKNG-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H19ClN4O4/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28)
Chemical Name
4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide
Synonyms
E-7080; E7080; E 7080; ER-203492-00; Lenvatinib; Brand name: Lenvima
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~40 mg/mL (~93.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
0.5% methylcellulose: 30 mg/kg
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3427 mL 11.7137 mL 23.4274 mL
5 mM 0.4685 mL 2.3427 mL 4.6855 mL
10 mM 0.2343 mL 1.1714 mL 2.3427 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04447755 Active
Recruiting
Drug: Lenvatinib Relapsed or Refractory Solid
Tumors
Merck Sharp & Dohme LLC July 30, 2020 Phase 2
NCT04622566 Not yet recruiting Drug: Lenvatinib, Pembrolizumab Mucosal Melanoma
Neoadjuvant Treatment
Peking University Cancer
Hospital & Institute
December 30, 2020 Phase 2
NCT04297254 Recruiting Drug: Imatinib Mesylate Carcinoma, Hepatocellular Eisai Pharmaceuticals India
Pvt. Ltd
February 4, 2021 Phase 4
NCT05308901 Recruiting Drug: Lenvatinib
Drug: Pembrolizumab
Melanoma, Uveal Providence Health & Services August 2, 2022 Phase 2
NCT04519151 Recruiting Drug: Lenvatinib
Drug: Pembrolizumab
Ovarian Neoplasms
Ovarian Diseases
Sheba Medical Center April 12, 2021 Phase 2
Biological Data
  • Kinase inhibitory profile of E7080. Int J Cancer . 2008 Feb 1;122(3):664-71.
  • Effect of E7080 on SCF- and VEGF-induced angiogenesis in the sandwich tube formation (sTF) assay. Int J Cancer . 2008 Feb 1;122(3):664-71.
  • Comparison of effects of E7080 and imatinib on SCF- and VEGF-induced angiogenesis in the sandwich tube formation (sTF) assay. Int J Cancer . 2008 Feb 1;122(3):664-71.
  • Effects of lenvatinib for ATC. Cancer Control . 2018 Jan-Dec;25(1):1073274818789361.
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