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Lenvatinib (E7080) (Synonyms: E-7080, ER-203492-00)

Catalog No.GC15454

Le lenvatinib (E7080) (E7080) est un inhibiteur de la tyrosine kinase oral À cibles multiples qui inhibe VEGFR1-3, FGFR1-4, PDGFR, KIT et RET, et présente de puissantes activités antitumorales.

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Lenvatinib (E7080) Chemical Structure

Cas No.: 417716-92-8

Taille Prix Stock Qté
10mM (in 1mL DMSO)
52,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Preparation Method

4μL of serial dilutions of Lenvatinib (E7080) were mixed in a 96-well round plate with 10μL of enzyme (KDR), 16μL of poly (GT) solution (250 ng) and 10μL of ATP solution (1μmol/L ATP) (final concentration of DMSO was 0.1%).The kinase reaction was initiated by adding ATP solution to each well. After 30-min incubation at 30°C, the reaction was stopped by adding 0.5 mol/L EDTA (10μL/well) to the reaction mixture in each well. HTRF solution (50μL/well) was added to the reaction mixture, and then kinase activity was determined by measurement of fluorescence with a time-resolved fluorescence detector at an excitation wavelength of 337 nm and an emission wave-lengths of 620 and 665 nm.

Reaction Conditions

4μL,30 min

Applications

Lenvatinib (E7080) inhibited KDR with IC50 values of 4.0 nM.

Cell experiment [2]:

Cell lines

8505C and TCO1 cell

Preparation Method

The cells were grown in 96-well microplates in a final volume of 100 μL culture medium per well. The cells were incubated with 0.1 to 50 μM Lenvatinib (E7080) for 48 h. Then, 50 μL of the XTT labeling mixture was added to each well to a final XTT concentration of 0.3 mg/mL. After incubation of the microplate for 4 h in 5% CO2 at 37 °C in a humidified incubator, the formazan dye formed was quantified using a scanning multiwell spectrophotometer.

Reaction Conditions

0.1 to 50 μM Lenvatinib (E7080) for 48 h

Applications

The half-maximal inhibitory concentrations (IC50) for Lenvatinib (E7080) treatment of 8505C and TCO1 cells were 24.26 and 26.32 μM, respectively.

Animal experiment [1]:

Animal models

Female BALB/c nude mice (8–12 weeks old, 20–25 g)

Preparation Method

H146 tumor cells (6.5×106) were implanted subcutaneously into the flank region of mice. Twelve days after inoculation, mice were randomized into control (n=12) and treatment groups (n=6) and this point in time was identified as day 1. Lenvatinib (E7080) were suspended in 0.5% methylcellulose and saline, and administered orally twice a day for Lenvatinib (E7080) from day 1 to day 21. Tumor volume was measured on the indicated days and calculated.

Dosage form

Administer orally twice a day for Lenvatinib (E7080)

Applications

Oral administration of Lenvatinib (E7080) inhibited the growth of H146 tumor at 30 and 100 mg/kg in a dose-dependent manner and caused tumor regression at 100 mg/kg.

References:

[1]. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M. 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 Feb 1;122(3):664-71.

[2]. Enomoto K, Hirayama S, Kumashiro N, Jing X, Kimura T, Tamagawa S, Matsuzaki I, Murata SI, Hotomi M. Synergistic Effects of Lenvatinib (E7080) and MEK Inhibitors against Anaplastic Thyroid Cancer in Preclinical Models. Cancers (Basel). 2021 Feb 18;13(4):862.

Background

E7080, known as lenvatinib, is an oral multitargeted tyrosine kinase inhibitor including VEGF, FGF and SCF receptors that has been shown to improve the survival rate of patients with radioiodine-refractory thyroid cancer. Lenvatinib (E7080) had antitumor activity against HCC PDX models, likely through its potent anti-angiogenic activity [1].

Lenvatinib (E7080) inhibited Flt-1, KDR, Flt-4 with IC50 values of 22, 4.0 and 5.2 nM, respectively. Lenvatinib (E7080) inhibited FGFR1 and FDGFR tyrosine kinases. In addition to these kinases, Lenvatinib (E7080) also inhibited KIT kinase with an IC50 value of 100 nM [2]. The half-maximal inhibitory concentrations (IC50 ) for Lenvatinib (E7080) treatment of 8505C and TCO1 cells were 24.26 and 26.32 μM, respectively [3].

The novel multi-targeted kinase inhibitor Lenvatinib (E7080), which inhibited both KDR and KIT kinases, showed a more potent antitumor efficacy against H146 tumor than imatinib. Oral administration of Lenvatinib (E7080) inhibited the growth of H146 tumor at 30 and 100 mg/kg in a dose-dependent manner and caused tumor regression at 100 mg/kg [2]. Lenvatinib (E7080) at 10 and 30 mg/kg inhibited the tumor growth of both PDXs, LI0050 and LI0334 [1]. Lenvatinib (E7080), as compared with placebo, was associated with significant prolongation of progression-free survival and an improved response rate (64.8% vs. 1.5%) among patients with iodine-131–refractory differentiated thyroid cancer [4].

References:
[1].Matsuki M, Hoshi T, Yamamoto Y, Ikemori-Kawada M, Minoshima Y, Funahashi Y, Matsui J. Lenvatinib inhibits angiogenesis and tumor fibroblast growth factor signaling pathways in human hepatocellular carcinoma models. Cancer Med. 2018 Jun;7(6):2641-2653.
[2].Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M. 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 Feb 1;122(3):664-71.
[3].Enomoto K, Hirayama S, Kumashiro N, Jing X, Kimura T, Tamagawa S, Matsuzaki I, Murata SI, Hotomi M. Synergistic Effects of Lenvatinib (E7080) and MEK Inhibitors against Anaplastic Thyroid Cancer in Preclinical Models. Cancers (Basel). 2021 Feb 18;13(4):862.
[4].Schlumberger M, Tahara M, Wirth LJ, Robinson B, Brose MS, Elisei R, Habra MA, Newbold K, Shah MH, Hoff AO, Gianoukakis AG, Kiyota N, Taylor MH, Kim SB, Krzyzanowska MK, Dutcus CE, de las Heras B, Zhu J, Sherman SI. Lenvatinib versus placebo in radioiodine-refractory thyroid cancer. N Engl J Med. 2015 Feb 12;372(7):621-30.

Chemical Properties

Cas No. 417716-92-8 SDF
Synonymes E-7080, ER-203492-00
Chemical Name 4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide
Canonical SMILES COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl
Formula C21H19ClN4O4 M.Wt 426.85
Solubility DMSO: 8.33 mg/mL (15.93 mM) Storage Store at 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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