Lenvatinib (E7080)

製品コードS1164

Lenvatinib (E7080)化学構造

分子量(MW):426.85

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. Phase 3.

サイズ 価格(税別)  
In DMSO JPY 51800
JPY 13600
JPY 26900
JPY 46800
JPY 129800
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バルク問合せ

カスタマーフィードバック(5)

  • Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.

    Asian Pac J Cancer Prev 2014 15(7), 3113-21. Lenvatinib (E7080) purchased from Selleck.

    Real-time monitoring of cytotoxic effect on HT29 cells using RTCA. (A) E7080

    Chin J Cancer Res 2013 25(5), 572-84. Lenvatinib (E7080) purchased from Selleck.

  • Calculation of IC50 of E7080 (IC50 =5.60×10–8 mol/L, square R =0.998).

    Chin J Cancer Res 2013 25(5), 572-84. Lenvatinib (E7080) purchased from Selleck.

    Tetrathiomolybdate (TM) reduces anchorage-independent growth of BCPAP cells. A, % transformed growth in soft agar (mean ± SEM, triplicate samples, three experiments) normalized to vehicle control of BCPAP cells treated with increasing doses (effective concentration) of lenvatinib (blue ▲), sorafenib (■),TM (●), vemurafenib (◆), or trametinib (△).

    Clin Cancer Res, 2018, 24(17):4271-4281. Lenvatinib (E7080) purchased from Selleck.

  • Inhibitors of tyrosine kinase receptor suppressed the in vitro angiogenesis of HUVECs. The angiogenesis of HUVECs was evaluated in the absence (control in A) or presence of CP-673451 (5 nM), a selective inhibitor of PDGFR or E7080 (50 nM), an active inhibitor for multiple tyrosine kinase receptors for 6 h. The two agents only inhibit the kinase activity of the relative tyrosine kinase receptors, but do not cause a toxic effect to the cells in the concentration used in this study (Roberts et al., 2005 ; Wiegering et al., 2014). For quantification, the values for the pattern recognition, branch point and total capillary tube length are described in the Methods section. Representative microscopic fields are shown in Panel A. The suppressive effects of the inhibitors on angiogenesis of HUVECs are shown in B, C and D. The data are expressed relative to that of the control cells without exposure to the inhibitor. N = 5, *P < 0.05 and **P < 0.01 versus the control cells.

    Environ Toxicol Pharmacol, 2016, 46:168-73. Lenvatinib (E7080) purchased from Selleck.

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

製品説明 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. Phase 3.
ターゲット
VEGFR2/KDR [1]
(Cell-free assay)
VEGFR3/FLT4 [1]
(Cell-free assay)
VEGFR1/FLT1 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
4.0 nM 5.2 nM 22 nM 39 nM 46 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TPC-1 and K1 cells MYfGeY5kfGmxbjDhd5NigQ>? MXG1NQKBkc7:TR?= M1jURVI1KGh? NIH5O4xVcGViaX7obYJqfG:{eTDl[oZm[3S|IH;mJIxmdn[jdHnubYIhd25idHjlJJZq[WKrbHn0fUBw\iCkb4ToJINmdGxibHnu[ZMhf2W{ZTDuc5QhcW6obIXlcoNm\CCkeTD0bIUhdGWydHnuJJRz\WG2bXXueE4> NGPvbWY{ODlyNkOyNS=>
ATC cells NHvyc5FHfW6ldHnvckBie3OjeR?= M{\TWlEtKDJ3IHHu[EA2OCEQvF2= MkXCO|IhcA>? M13WWXBpd3OyaH;yfYxifGWmL37vck1xcG:|cHjvdplt[XSnZDDBb5Qhd3JiRWLLNU8zKHC{b4TlbY5{KCindnHseYF1\WRiYomgSWxKW0FrIHnuJIxmdn[jdHnubYIufHKnYYTl[EB{[W2ybHXzJJdmemVic3nncolncWOjboTsfUBz\WS3Y3XkJIlvKEGWQzDj[YxtKGO3bIT1doV{Ng>? MmjNNlk2OTdzMEO=
HCC cell lines Hep3B2.1-7, HuH-7, and JHH-7 MU\Qdo9tcW[ncnH0bY9vKGG|c3H5 Mkn6OkBl[Xm| NUDrZZNYVGWwdnH0bY5q[iC|aH;3[YQhe2WuZXP0bZZmKGGwZDDwc5RmdnRiYX70bZBzd2yrZnXyZZRqfmViYXP0bZZqfHliYXfhbY5{fCC2aHWgTGNEKGOnbHygcIlv\XNiSHXwN2IzNjIkgKC3MEBJfUkkgKC3MEBidmRiSljI5qCRPyxid3n0bEBKSzVyII\hcJVmeyCxZjCwMlI{NCByLkSyMEBidmRiMD62OEDPxG2xbD;MMEBz\XOyZXP0bZZmdHlw M{HpOVI6PzN|NUGx
HT29 cells NHzsNodEgXSxdH;4bYNqfHliYYPzZZk> MXSyOUwhPTBibl2= NYHhcJBzPzJiaB?= MVfjfZRwfG:6aXOg[I9{\TpiNUCgcm0h[W6mIH7vcoN6fG:2b4jpZ{Bld3OnOjCyOUBvVQ>? NXvOUlhSOjR6MUW0OVY>
DX3 and U2OS cells NU\6NXFuTnWwY4Tpc44h[XO|YYm= Ml\ENUDPxE1iYX7kJFExKM7:TR?= MXSxOkBpd3W{cx?= Mmm1UIVvfmG2aX7pZkBqdmirYnn0JJR2dW:{IHPlcIx{KG2rZ4LheIlwdiCjbnSgbY53[XOrb36gZZQh[2:wY3XueJJifGmxboOgeIhifCCkb4ToJIlvcGmkaYSgbZR{KGuwb4fuJJRiemendIOgZY5lKGG{ZTDhZ4hq\X[jYnzlJINtcW6rY3HscJkv NFPCNWkzOTd6MUOxOy=>

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アッセイ
Methods Test Index PMID
Western blot
phospho-FGFR1 / FGFR1 /phospho-FRS2 / FRS2 / phospho-MEK / phospho-ERK; 

PubMed: 25295214     


Effect of lenvatinib on FGFR1 signaling pathway in human DTC RO82-W-1 cells in vitro. After starvation overnight, RO82-W-1 cells were treated with vehicle (control), lenvatinib or sorafenib at the indicated concentrations for 1 h and were then stimulated for 10 min with bFGF (20 ng/mL) and heparin before being lysed. Western blot analyses of the phosphorylation of FGFR1 and its downstream effectors in RO82-W-1 cells were then performed and representative images were shown.

phospho-RET; 

PubMed: 25295214     


Western blot analyses of the phosphorylation of RET in human medullary thyroid TT cells. TT cells were seeded and cultured overnight. They were then treated with lenvatinib at the indicated concentrations for 1 h before being lysed.

Ki-67 / Cyclin D1 / CDK4 / p21 / p53 / Apaf-1 / p-NFκB / Bcl-2 / Cleaved-caspase 3; 

PubMed: 30286728     


Immunoblot analysis of cell-cycle arrest and apoptotic proteins in the advanced PTC cell line.

β-catenin; 

PubMed: 30286728     


(a and c) Immunofluorescence assay for nuclear translocation of β-catenin. Results confirmed that SoLAT inhibited nuclear translocation of β-catenin in the advanced PTC cells more potently than either agent alone.

Vimentin / E-cadherin / Snail / Zeb1; 

PubMed: 30286728     


(b and d) Immunoblot analysis of EMT markers showed that most EMT markers such as vimentin, E-cadherin, Snail, and Zeb1 were inhibited by FGFR inhibition (p-ERK1/2) in the SoLAT group.

25295214 30286728
Growth inhibition assay
Cell viability; 

PubMed: 25425971     


Dose-response effects of E7080 on cell viability of human colorectal carcinoma (CRC) cells and endothelial cells (HUVEC). IC50 values were determined in serum reduced (1%) RPMI 1640 medium following treatment with different concentrations of E7080 for 72 hours. The final concentration of DMSO (vehicle) was ≤1%. Results are expressed as the mean ± S.E.M. of at least three independent proliferation assays with hexaplicates.

25425971
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [2]
+ 展開
  • 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. 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.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: H146 tumor cells are implanted subcutaneously (s.c.) into the flank region of female BALB/c nude mice.
  • 製剤: E7080 is dissolved in suspended in 0.5% methylcellulose.
  • 投薬量: ≤100 mg/kg
  • 投与方法: Administered via p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 40 mg/mL (93.7 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
0.5% methylcellulose
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 426.85
化学式

C21H19ClN4O4

CAS No. 417716-92-8
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03841201 Not yet recruiting Advanced Hepatocellular Carcinoma IKF Klinische Krebsforschung GmbH at Krankenhaus Nordwest|Bristol-Myers Squibb|Eisai GmbH April 2019 Phase 2
NCT03744247 Not yet recruiting Hepatocellular Carcinoma Sun Yat-sen University|First Affiliated Hospital Sun Yat-Sen University|Kaiping Central Hospital|Guangzhou No.12 People''s Hospital|The First Affiliated Hospital of University of South China April 21 2019 Phase 3
NCT03324373 Not yet recruiting Renal Cell Carcinoma Yousef Zakharia|Eisai Research Institute|University of Iowa April 30 2019 Phase 1
NCT03841201 Not yet recruiting Advanced Hepatocellular Carcinoma IKF Klinische Krebsforschung GmbH at Krankenhaus Nordwest|Bristol-Myers Squibb|Eisai GmbH April 2019 Phase 2
NCT03744247 Not yet recruiting Hepatocellular Carcinoma Sun Yat-sen University|First Affiliated Hospital Sun Yat-Sen University|Kaiping Central Hospital|Guangzhou No.12 People''s Hospital|The First Affiliated Hospital of University of South China April 21 2019 Phase 3
NCT03324373 Not yet recruiting Renal Cell Carcinoma Yousef Zakharia|Eisai Research Institute|University of Iowa April 30 2019 Phase 1

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID