Lenvatinib (E7080)

製品コードS1164 バッチS116406

印刷

化学情報

Synonyms

E7080

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₁₉ClN₄O₄

分子量

426.85

CAS No.

417716-92-8

Solubility (25°C)*

体外

DMSO

50 mg/mL (117.13 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/ml (1.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	レンバチニブ (Lenvatinib (E7080)) はマルチターゲット阻害剤の一種であり、主に VEGFR2(KDR)/VEGFR3(Flt-4) に対して活性を示し IC50 は 4 nM/5.2 nMである一方、VEGFR1/Flt-1に対しては活性が弱く、cell-free assay において FGFR1, PDGFRα/βよりも VEGFR2/3 に対して 10 倍高い選択性を示します。レンバチニブ (E7080) はまた FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET) も阻害し、強力な抗腫瘍活性を呈します。
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, this compound inhibits Flt-1, KDR, Flt-4 with IC50 of 22, 4.0 and 5.2 nM, respectively. In addition to these kinases, this compound also inhibits FGFR1 and PDGFR tyrosine kinases with IC50 value of 46, 51 and 100 nM for FGFR1, PDGFRα and PDGFRβ, respectively. ^[1] This compound 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 this compound 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]
in vivo	When orally administrated in a H146 xenograft model, Lenvatinib (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, this compound at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and imatinib treatment. ^[1] It 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]

プロトコル(参考用のみ)

キナーゼアッセイ	In vitro kinase assay ^[1]
キナーゼアッセイ	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 this compound 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.
細胞アッセイ	細胞株	HUVECs
	濃度	0-10 μM
	反応時間	72 hours
	実験の流れ	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. This compound 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.
動物実験	動物モデル	H146 tumor cells are implanted subcutaneously (s.c.) into the flank region of female BALB/c nude mice.
	投薬量	≤100 mg/kg
	投与方法	Administered via p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/17943726/
https://pubmed.ncbi.nlm.nih.gov/18765537/
https://pubmed.ncbi.nlm.nih.gov/21781317/

https://pubmed.ncbi.nlm.nih.gov/24190702/

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カスタマーフィードバック

: Data from [Data independently produced by Asian Pac J Cancer Prev, 2014, 15(7), 3113-21]

: Data from [Chin J Cancer Res, 2013, 25(5), 572-84]

: Data from [Chin J Cancer Res, 2013, 25(5), 572-84]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Human-correlated genetic models identify precision therapy for liver cancer [ Nature, 2025, 10.1038/s41586-025-08585-z]	PubMed: 39972137
DTX2 attenuates Lenvatinib-induced ferroptosis by suppressing docosahexaenoic acid biosynthesis through HSD17B4-dependent peroxisomal β-oxidation in hepatocellular carcinoma [ Drug Resist Updat, 2025, 81:101224]	PubMed: 40058099
Androgen receptor promotes arachidonic acid metabolism and angiogenic microenvironment in AFP-negative hepatocellular carcinoma [ Nat Commun, 2025, 16(1):6451]	PubMed: 40651942
NEK7-induced phosphorylation of EGFR on serine 1070 drives the acquired lenvatinib resistance in hepatocellular carcinoma [ Hepatology, 2025, 10.1097/HEP.0000000000001474]	PubMed: 40694824
Dual-responsive magnetic vortex nanorings co-deliver lenvatinib and localized heat for synergistic activation of antitumor immunity [ Acta Biomater, 2025, 198:389-400]	PubMed: 40204172
GPX2 inhibition enhances antitumor efficacy of lenvatinib via promoting immunogenic cell death in hepatocellular carcinoma [ J Transl Med, 2025, 23(1):456]	PubMed: 40251668
Relevance of transportome among the mechanisms of chemoresistance in hepatoblastoma [ Biochem Pharmacol, 2025, 237:116914]	PubMed: 40185314
Arsenic trioxide enhances the inhibitory effect of lenvatinib on hepatocellular carcinoma through HMOX1-mediated ferroptosis [ Int Immunopharmacol, 2025, 167:115656]	PubMed: 41072079
The SCD1 inhibitor aramchol interacts with regorafenib to kill GI tumor cells in vitro and in vivo [ Oncotarget, 2025, 16:662-678]	PubMed: 40827882
Precision-cut tumor slices for modeling hepatocellular carcinoma enable at-scale drug screening [ Hepatol Commun, 2025, 9(6)e0706]	PubMed: 40377490

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。