Nintedanib (BIBF 1120)

製品コードS1010 別名:Intedanib

Nintedanib (BIBF 1120)化学構造


Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

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  • 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.

    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.

    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.

  • Immunofluorescence Assay. PDCD4, GRA3, and overlapping are represented in red, green, and yellow, respectively. Group I TKIs sunitinib and AZD9291 show similar results to that of the negative control with PDCD4 and GRA3 well localized inside the nuclei. Mild disruption of PDCD4 in the nuclei is observed with Group II TKIs gefitinib, erlotinib, and AG1478. Group III TKIs neratinib, afatinib, and pelitinib show comparable changes to that of pyrimethamine 5 μM, with complete disruption of PDCD4 and GRA3, without any localization. The assays were repeated 3 times, and each experiment was performed in triplicate. A representative result is shown (x1,000).

    Korean J Parasitol, 2017, 55(5): 491-503. 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.




製品説明 Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.
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

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]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 NIfZUXVHfW6ldHnvckBCe3OjeR?= NITLWXU2KML3TR?= MljrNlQhcA>? MVvEUXNQ NYjlWlNpcW6mdXPld{BiKHOrZ37p[olk[W62IHnuZ5Jm[XOnIHnuJJRp\SCycn;tc5RmeiCjY4Tpeol1cWW|IH;mJGUu[2GmLNMgR2RJOSxiYX7kxsBETEh| NHHxeYkzPjB4MUe0Oy=>
A549 M1vUbmZ2dmO2aX;uJGF{e2G7 NYnBTG9xOi93IN88US=> NUj0WG5JOjRiaB?= NF25O3FFVVOR M4nHWIhieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg NV31[4R7OjZyNkG3OFc>
Mia-Paca2 NWm3UVViTnWwY4Tpc44hSXO|YYm= NIKwU|UzNzVizszN NEjMdYUzPCCq MXTEUXNQ M17SeohieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg NWDnOlJ4OjZyNkG3OFc>
A549 MYLGeY5kfGmxbjDBd5NigQ>? M2f1WVAvODIkgKO1xsDPxE1? MkGzNlQhcA>? M3Tn[GROW09? MXTpcoR2[2W|IGPGWHBFyqCvUl7BJIV5eHKnc4Ppc44h\G:|ZTDk[ZBmdmSnboTsfS=> M3XnZVI2QDR|MEC1
A549 MoXNSpVv[3Srb36gRZN{[Xl? NGTpSJAxNjBz4pETOeKh|ryP M{[zXVczKGh? NWjEb|k1TE2VTx?= MXLlcohidmOnczDTVE1FKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meiCjdDDjc45k\W62cnH0bY9veyCxZjD1dEB1dyB3wrFOwG3DqA>? M{nzNFI2QDR|MEC1
A549 M4fiPGZ2dmO2aX;uJGF{e2G7 M2LhWlXDqM7:TR?= MlnJNE0yKGh? M4rmVWROW09? M1TIW4lv[3KnYYPld{BCWC1zIHHjeIl3[XSrb36gJIFnfGW{IEOwJI1qdg>? MXyyOVg1OzByNR?=
Hep3B Mn:0R4VtdCCYaXHibYxqfHliQYPzZZk> MlHzNE0zOCEQvF2= NID2dGo1QMLiaB?= MWnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M1\O[VI1PjV5M{m4
HepG2 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXXJdVlWOC1{MDFOwG0> NGKxZXQ1QMLiaB?= M3fjXIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlXKNlQ3PTd|OUi=
PLC5 NYP4VYVMS2WubDDWbYFjcWyrdImgRZN{[Xl? M2rBN|AuOjBizszN NFzVfYg1QMLiaB?= M{DoPYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Mo[xNlQ3PTd|OUi=
HuH7 MoPCR4VtdCCYaXHibYxqfHliQYPzZZk> NFm0VWExNTJyIN88US=> MWO0POKhcA>? NYnL[oY1\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= MmrhNlQ3PTd|OUi=
SK-Hep1 M1;PbWNmdGxiVnnhZoltcXS7IFHzd4F6 NX7vR2RqOC1{MDFOwG0> MYe0POKhcA>? NFmxS45l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MkLYNlQ3PTd|OUi=
Hep3B Mlj6RZBweHSxc3nzJGF{e2G7 NYfYRnFpOC1{MDFOwG0> MXy0POKhcA>? M1HRfIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? MV:yOFY2PzN7OB?=
HepG2 NHfveGNCeG:ydH;zbZMhSXO|YYm= MWOwMVIxKM7:TR?= NUPNcZU{PDkEoHi= NHvO[HhqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHTvd4Uh\GWyZX7k[Y51dHl? NILVcpEzPDZ3N{O5PC=>
PLC5 MWLBdI9xfG:|aYOgRZN{[Xl? NXfwOlNQOC1{MDFOwG0> NYjvTop5PDkEoHi= MnXPbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NXq0SolFOjR4NUezPVg>
HuH7 NYrle21lSXCxcITvd4l{KEG|c3H5 MV6wMVIxKM7:TR?= NGHPdFA1QMLiaB?= NWHzUXN2cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NHnFRpAzPDZ3N{O5PC=>
SK-Hep1 MV3BdI9xfG:|aYOgRZN{[Xl? NGDyfW8xNTJyIN88US=> MV:0POKhcA>? NXLMZWlocW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M4m5WVI1PjV5M{m4
H1703 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrKeHJKSzVyPUCuNFUh|ryP NXz3T2NnOjN5Mkm0NFM>


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]


+ 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.
+ 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.

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 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):
5% DMSO+40% PEG 300+2% Tween 80+ddH2O

* 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。


分子量 539.62


CAS No. 656247-17-5
in solvent
別名 Intedanib





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


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


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

  • C1



  • 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):




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


質量 濃度 体積 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02835833 Completed Renal Cell Carcinoma|Colorectal Adenocarcinoma|Non-squamous Non-small Cell Lung Cancer|Platinum-refractory Ovarian Carcinoma|Cervical Carcinoma University of Alabama at Birmingham|Boehringer Ingelheim June 9 2016 Phase 1
NCT02788474 Completed Idiopathic Pulmonary Fibrosis Boehringer Ingelheim June 9 2016 Phase 4
NCT02393755 Active not 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
NCT02902484 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 September 7 2017 Phase 1|Phase 2
NCT02808247 Recruiting Sarcoma Soft Tissue European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim July 7 2017 Phase 2
NCT02668393 Recruiting Carcinoma Non-Small-Cell Lung Boehringer Ingelheim March 7 2016 Phase 1



Handling Instructions


  • * 必須


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