Nintedanib (BIBF 1120)

製品コードS1010 別名:Intedanib

Nintedanib (BIBF 1120)化学構造

分子量(MW):539.62

Nintedanib (BIBF 1120)は一種の有効な三重血管キナーゼ阻害剤で、無細胞試験でVEGFR1/2/3、FGFR1/2/3とPDGFRα/βに作用する時のIC50値が34 nM/13 nM/13 nM、69 nM/37 nM/108 nMと59 nM/65 nMにそれぞれ分かれることです。臨床3期。

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JPY 39840.00
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カスタマーフィードバック(7)

  • PBLs from CLL5 were treated with vehicles (0.1% ethanol and 0.005% DMSO), 106 M dexamethasone, 50 nM BIBF 1120, or both for 24 h. Cells were also treated with 0.1% ethanol or 106 M dexamethasone in the presence of either nonphosphorylated (control) EGQYEEIP or phosphorylated EGQY*EEIP H2O soluble peptides (200 nM) for 24 h.

     

     

    Cell Death Differ 2010 17, 1381-1391. Nintedanib (BIBF 1120) purchased from Selleck.

    Nintedanib decreases constitutive expression of extracellular matrix proteins fibronectin and collagen 1a1 in idiopathic pulmonary fibrosis (IPF) fibroblasts. (A and B) IPF fibroblasts were treated with increasing doses of nintedanib (0.5, 1, or 2 μM) (A) or nintedanib (2 μM) for increasing durations (24, 48, or 72 h) (B). Expression of fibronectin and collagen 1a1 was evaluated by Western immunoblotting.

    Am J Respir Cell Mol Biol, 2016, 54(1):51-9. Nintedanib (BIBF 1120) purchased from Selleck.

  • Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

    Effect of BIBF 1120 on the expression of ABCB1 in MDR cells. Hep G2/adr and MCF-7/adr cells were treated with BIBF 1120 at various concentrations for 48 h. a The mRNA level of ABCB1 was determined by RT-PCR as described in "Materials and Methods"; b Equal amounts of total cell lysates were loaded and detected by Western blot. A representative result is shown from at least three independent experiments

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

  • Effect of BIBF 1120 on blockade of AKT and ERK1/2 phosphorylation. Hep G2/adr and MCF-7/adr cells were treated with drugs for 24 h. Equal amount of protein was loaded for Western blot as described in "Materials and Methods". All these experiments were repeated at leas thrice, and a representative experiment is shown in each pane

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

    BIBF 1120 inhibition of verapamil-stimulated ABCB1 ATPase activity. ABCB1 ATPase assays were performed according to the instruction of Pgp-Glo™ Assay Systems. Each point represents the mean±SDs for triplated independent determinations

    Cell Oncol 2011 34, 33–44. Nintedanib (BIBF 1120) purchased from Selleck.

  • Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (±SD) from 3 experiments.

     

     

    AACR 2011 Nintedanib (BIBF 1120) 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 Nintedanib (BIBF 1120)は一種の有効な三重血管キナーゼ阻害剤で、無細胞試験でVEGFR1/2/3、FGFR1/2/3とPDGFRα/βに作用する時のIC50値が34 nM/13 nM/13 nM、69 nM/37 nM/108 nMと59 nM/65 nMにそれぞれ分かれることです。臨床3期。
ターゲット
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
LCK [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
VEGFR1 [1]
(Cell-free assay)
13 nM 13 nM 16 nM 26 nM 34 nM
体外試験

BIBF1120 inhibits PDGFR kinase activity of PDGFR alpha and PDGFR beta types with IC50 values of 59 nM and 65 nM, respectively. In addition, BIBF1120 suppresses the FGFR subtypes with IC50 of 60 nM, 37 nM and 108 nM for FGFR1, FGFR2, and FGFR3, respectively. BIBF1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. The indolinone scaffold forms two hydrogen bonds with the backbone nitrogen of Cys919 and the backbone carbonyl oxygen of Glu917 in the hinge region. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 at concentrations as low as 100 nM blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. In cultures of human vascular smooth muscle cells (HUASMC), BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 MmPjSpVv[3Srb36gRZN{[Xl? MW[1JOK2VQ>? NV65XZJnOjRiaB?= NHW2R3JFVVOR NHHNdnlqdmS3Y3XzJIEhe2mpbnnmbYNidnRiaX7jdoVie2ViaX6geIhmKHC{b33veIVzKGGldHn2bZRq\XNib3[gSU1k[WRuwrDDSGgyNCCjbnVCpGNFUDN? M4C2NlI3ODZzN{S3
A549 MWXGeY5kfGmxbjDBd5NigQ>? M2foVVIwPSEQvF2= M{i0NFI1KGh? MoK1SG1UVw>? M{XJ[IhieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg MVSyOlA3OTd2Nx?=
T24 NHfrV|FHfW6ldHnvckBCe3OjeR?= M4ToPFIwPSEQvF2= Mn[xNlQhcA>? M1X5UmROW09? MlP6bIF{KGFiZ3Xu[ZJidCCHTWSgdoV3\XK|YXyg[YZn\WO2wrC= MlHINlYxPjF5NEe=
Mia-Paca2 NGnjZppHfW6ldHnvckBCe3OjeR?= NFnqOo8zNzVizszN MlWzNlQhcA>? NH;wOW5FVVOR Mo\3bIF{KGFiZ3Xu[ZJidCCHTWSgdoV3\XK|YXyg[YZn\WO2wrC= NYHKemZsOjZyNkG3OFc>
A549 MmmwSpVv[3Srb36gRZN{[Xl? MXSwMlAy6oDVNdMg{txO NFfte5QzPCCq NHjFNppFVVOR M33UZolv\HWlZYOgV2ZVWEUEoH3SUmEh\XiycnXzd4lwdiCmb4PlJIRmeGWwZHXueIx6 Mo\CNlU5PDNyMEW=
A549 NYDoWYRHTnWwY4Tpc44hSXO|YYm= M1vOfVAvODIkgKO1xsDPxE1? M4HjdlczKGh? MYXEUXNQ NXvROVRx\W6qYX7j[ZMhW1BvRDDwdo91\WmwIHX4dJJme3Orb36gbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZZQh[2:wY3XueJJifGmxboOgc4YhfXBidH:gOeKh|ryPwrC= M3;oXVI2QDR|MEC1
A549 MX7GeY5kfGmxbjDBd5NigQ>? M3PFRlXDqM7:TR?= NEHEfWMxNTFiaB?= Ml63SG1UVw>? MYjpcoNz\WG|ZYOgRXAuOSCjY4TpeoF1cW:wIDDh[pRmeiB|MDDtbY4> MoDLNlU5PDNyMEW=
Hep3B NEPvTFBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4HveVAuOjBizszN MlGzOFjDqGh? NW\ZT4Ft\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= MYKyOFY2PzN7OB?=
HepG2 NUTtcG55S2WubDDWbYFjcWyrdImgRZN{[Xl? MV2wMVIxKM7:TR?= MXW0POKhcA>? NIXENnNl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MX[yOFY2PzN7OB?=
PLC5 NHuwXWdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmrlNE0zOCEQvF2= M3T0cVQ5yqCq MVjk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NU\uTHgyOjR4NUezPVg>
HuH7 NWn1S5pCS2WubDDWbYFjcWyrdImgRZN{[Xl? NXzFR5J4OC1{MDFOwG0> NHvJUmo1QMLiaB?= M4e2TIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NVXlOGQ1OjR4NUezPVg>
SK-Hep1 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NX3BblVsOC1{MDFOwG0> NWTwV3ZPPDkEoHi= NGXGTJdl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MmPGNlQ3PTd|OUi=
Hep3B MX3BdI9xfG:|aYOgRZN{[Xl? NEHLbpIxNTJyIN88US=> Moi1OFjDqGh? MXjpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> MlS5NlQ3PTd|OUi=
HepG2 MniyRZBweHSxc3nzJGF{e2G7 MWqwMVIxKM7:TR?= NXzVUFdMPDkEoHi= MorCbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 MmHvNlQ3PTd|OUi=
PLC5 NFPO[JRCeG:ydH;zbZMhSXO|YYm= NGr1UpkxNTJyIN88US=> M4K2OFQ5yqCq Mor1bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 MUGyOFY2PzN7OB?=
HuH7 MUnBdI9xfG:|aYOgRZN{[Xl? MYWwMVIxKM7:TR?= MoHaOFjDqGh? MUnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> MXmyOFY2PzN7OB?=
SK-Hep1 MYPBdI9xfG:|aYOgRZN{[Xl? MYmwMVIxKM7:TR?= MmLIOFjDqGh? NV\NTHJOcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MYCyOFY2PzN7OB?=
H1703 NIm3N|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMEWg{txO NIfZZo4zOzd{OUSwNy=>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 In all tumor models tested thus far, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model, BIBF1120 is highly active at well-tolerated doses (25-100 mg/kg daily p.o.). This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[3]
+ 展開

VEGFR2 Kinase Assay:

The cytoplasmic tyrosine kinase domain of VEGFR2 (residues 797-1355 according to sequence deposited in databank SWISS-PROT P35968) is cloned into pFastBac fused to GST and extracted. Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl2, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three washes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution.
細胞試験: [1]
+ 展開
  • 細胞株: HUVEC, HUASMC, and BRP cell lines
  • 濃度: 50 nM
  • 反応時間: 2 hours
  • 実験の流れ: The cell lines HUVEC, HUASMC, and BRP are used for the assay. BIBF1120 is added to the cultures two hours before the addition of ligands. Cell lysates are generated. Western blotting is done using standard SDS-PAGE methods, loading 50 to 75 μg of protein per lane. Detection is facilitated by enhanced chemiluminescence. Total and phosphorylated mitogen-activated protein kinase (MAPK) is analyzed using monoclonal antibodies M3807 and M8159. Total Akt is detected using the corresponding polyclonal antibody and phosphorylated Akt (Ser473) is analyzed by using its monoclonal antibody. Monoclonal antibody is also used to detect cleaved caspase-3 while KDR (VEGFR2) protein is detected using a corresponding antibody.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 xenografts in Athymic NMRI-nu/nu female mice
  • 製剤: In a 0.5 % Natrosol solution
  • 投薬量: 100 mg/kg
  • 投与方法: p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 6 mg/mL (11.11 mM)
Ethanol 3 mg/mL (5.55 mM)
Water Insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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 539.62
化学式

C31H33N5O4

CAS No. 656247-17-5
保管
別名 Intedanib

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02393755 Recruiting Colon Adenocarcinoma|Rectal Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|Boehringer Ingelheim|National Comprehensive Cancer Network May 8, 2015 Phase 1|Phase 2
NCT02863055 Not yet recruiting Malignant Pleural Mesothelioma European Organisation for Research and Treatment of Cancer - EORTC February 2017 Phase 2
NCT02999178 Recruiting Lung Diseases, Interstitial Boehringer Ingelheim January 2017 Phase 3
NCT02902484 Not yet recruiting Cancer of Pancreas University of Texas Southwestern Medical Center|Boehringer Ingelheim|The University of Texas Health Science Center at San Antonio|South Plains Oncology Consortium January 2017 Phase 1|Phase 2
NCT02808247 Not yet recruiting Sarcoma, Soft Tissue European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim January 2017 Phase 2
NCT02856867 Not yet recruiting Esophagogastric Adenocarcinoma|Metastatic Disease|No Previous Chemotherapy for Metastatic Esophagogastric Cancer European Organisation for Research and Treatment of Cancer - EORTC December 2016 Phase 2

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

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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