Lenvatinib (Synonyms: E7080)

製品番号: HY-10981 純度: 99.84%: FAQs
Data Sheet SDS COA 取扱説明書

Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Lenvatinib 構造式

CAS 番号 : 417716-92-8

容量	価格（税別）	在庫状況	数量

無料サンプル (0.1 - 0.5 mg)		今すぐ申し込む
Solution
10 mM * 1 mL in DMSO	USD 55	在庫あり	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 55	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	在庫あり	Estimated Time of Arrival: December 31
10 mg	USD 70	在庫あり	Estimated Time of Arrival: December 31
50 mg	USD 150	在庫あり	Estimated Time of Arrival: December 31
100 mg	USD 228	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 32 publication(s) in Google Scholar

Other Forms of Lenvatinib:

Lenvatinib mesylate 在庫あり

顧客検証

IHC

Proliferation Assay

RT-PCR

: Lenvatinib purchased from MCE. Usage Cited in: J Transl Med. 2022 Mar 7;20(1):116. [Abstract]; H&E examination of vehicle and Lenvatinib (10 mg/kg daily by oral gavage)-treated tumors revealed markedly increase tumor necrosis and desmoplasia in the Lenvatinib-treated samples.

: Lenvatinib purchased from MCE. Usage Cited in: J Oncol. 2022 Oct 18;2022:4537343.; HepG2 and HepG2/R cells are treated with or without Lenvatinib (20 μM) for 24 h, and indicated proteins are measured by western blots.

: Lenvatinib purchased from MCE. Usage Cited in: J Oncol. 2022 Oct 18;2022:4537343.; HepG2 and HepG2/R cells are treated with indicated doses of Lenvatinib for 24 h, and cellular viabilities are measured.

: Lenvatinib purchased from MCE. Usage Cited in: Cell Death Discov. 2021 Nov 18;7(1):359. [Abstract]; Lenvatinib (1000 nM) has demonstrated the ability to significantly inhibit cell proliferation, and knockout of NF1 and DUSP9 significantly blocks the ability of lenvatinib to inhibit cell proliferation as well as the effect on cell number.

: Lenvatinib purchased from MCE. Usage Cited in: J Cell Mol Med. 2021 Jan;25(1):549-560. [Abstract]; The mRNA expression of VEGFR2 in HepG2-WT/Lenvatinib (LR; 5 μM) and Huh7-WT/LR cells. VEGFR2 mRNA expression is up-regulated in HepG2-LR and Huh7LR cells.

: Lenvatinib purchased from MCE. Usage Cited in: J Cell Mol Med. 2021 Jan;25(1):549-560. [Abstract]; The cell viability is measured by CCK-8 assay at different time intervals (24, 48, 72 and 96 h) when cells are cultured with 5 μM Lenvatinib.

: Lenvatinib purchased from MCE. Usage Cited in: J Cell Mol Med. 2021 Jan;25(1):549-560. [Abstract]; The protein expression of VEGFR2 in HepG2-WT/Lenvatinib (LR; 5 μM) and Huh7-WT/LR cells. Western blotting results show the downstream target RAS/MEK/ERK axis of VEGFR2 are obviously up‐regulated in HepG2-LR and Huh7-LR cells compared with their parental cells.

VEGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

FGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

PDGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PDGFR PDGFRβ PDGFRα

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities^[1]^[2].

IC₅₀ & Target^[1]^[2]^[3]

VEGFR1

22 nM (IC₅₀)

VEGFR2

4 nM (IC₅₀)

VEGFR3

5.2 nM (IC₅₀)

FGFR1

46 nM (IC₅₀)

FGFR2

FGFR3

FGFR4

PDGFRα

51 nM (IC₅₀)

PDGFRβ

39 nM (IC₅₀)

c-Kit

100 nM (IC₅₀)

RET

体外実験

Lenvatinib (E7080) has IC₅₀s of 4, 5.2, 22 nM for VEGFR2 (KDR), VEGFR3 (Flt-4), and VEGFR1 (Flt-1), respectively. Lenvatinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC₅₀s of 51, 39, 46, and 100 nM, respectively^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Lenvatinib (E7080) (100 mg/kg, p.o.) significantly inhibits local tumor growth at the m.f.p., and at the end of treatment, Lenvatinib mesylate also significantly inhibits metastasis to both regional lymph nodes and distant lung^[3].
Lenvatinib (E7080) inhibits the growth of H146 tumor at 30 and 100 mg/kg (BID, QDx21) in a dose-dependent manner and causes tumor regression at 100 mg/kg in H146 xenograft model. IHC analysis with anti-CD31 antibody shows that lenvatinib at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and STI571 treatment^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

分子量

426.85

Appearance

Solid

分子式

C₂₁H₁₉ClN₄O₄

CAS 番号

417716-92-8

SMILES

O=C(N)C1=C(C=C2N=CC=C(C2=C1)OC3=CC=C(C(Cl)=C3)NC(NC4CC4)=O)OC

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : ≥ 12.78 mg/mL (29.94 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

*Please refer to the solubility information to select the appropriate solvent.

体内:

1.

Add each solvent one by one: 0.5% Methylcellulose/saline water
Solubility: 6.67 mg/mL (15.63 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 0.64 mg/mL (1.50 mM); Clear solution

*All of the co-solvents are available by MCE.

純度とドキュメンテーション

純度: 99.84%

Select Batch:

データシート (279 KB) SDS (251 KB)

COA (248 KB) HNMR (288 KB) LCMS (265 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Kudo M, et al. 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. [Content Brief]

[2]. Suyama K, et al. Lenvatinib: A Promising Molecular Targeted Agent for Multiple Cancers. Cancer Control. 2018 Jan-Dec;25(1):1073274818789361. [Content Brief]

[3]. Matsui J, et al. 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. [Content Brief]

[4]. Matsui J, et al. 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. [Content Brief]

細胞実験 ^[1]	H146 (1.2×10³ cells/50 μL/well) in SFM containing 0.5% BSA are cultured in 96-well multi-plates. After overnight culture at 37°C, SFM (150 μL/well) containing 0.5% FBS and several concentrations of SCF are added with or without several concentrations of compound. After culture for 72 hr, the ratios of surviving cells are measured by WST-1. MCE はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	Female BALB/c nude mice (8-12 weeks old, 20-25 g) are maintained under clean-room conditions. H146 tumor cells (6.5×10⁶) are implanted subcutaneously (s.c.) into the flank region of mice. Twelve days after inoculation, mice are randomized into control (n=12) and treatment (n=6 or n=5) groups and this point in time is identified as day 1. Lenvatinib and STI571, and VEGF neutralization antibody are suspended in 0.5% methylcellulose and saline, respectively, and administered orally twice a day for lenvatinib and STI571 and twice a week for antibody from day 1 to day 21. Tumor volume is measured on the indicated days and calculated. Antitumor activity is shown as a relative tumor volume (RTV=calculated tumor volume at indicated days/volume on day 1). MCE はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Kudo M, et al. 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. [Content Brief] [2]. Suyama K, et al. Lenvatinib: A Promising Molecular Targeted Agent for Multiple Cancers. Cancer Control. 2018 Jan-Dec;25(1):1073274818789361. [Content Brief] [3]. Matsui J, et al. 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. [Content Brief] [4]. Matsui J, et al. 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. [Content Brief]

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Lenvatinib417716-92-8E7080E 7080E-7080VEGFRFGFRPDGFRc-KitRETVascular endothelial growth factor receptorFibroblast growth factor receptorPlatelet-derived growth factor receptorSCFRCD117Inhibitorinhibitorinhibit

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Lenvatinib (Synonyms: E7080)

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Lenvatinib (Synonyms: E7080)

カスタマーレビュー

Other Forms of Lenvatinib:

顧客検証

おすすめ

•関連スクリーニングライブラリ:

VEGFR アイソフォーム固有の製品をすべて表示:

FGFR アイソフォーム固有の製品をすべて表示:

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生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

モル濃度カルキュレーター

希釈カルキュレーター

The molarity calculator equation

The dilution calculator equation

Keywords:

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