Nintedanib (BIBF 1120)

For research use only. Not for use in humans.

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.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 41800 あり
JPY 21900 あり
JPY 36800 あり
JPY 113200 あり

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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 MYfGeY5kfGmxbjDBd5NigQ>? NHL3N4o2KML3TR?= MlH5NlQhcA>? M3nhZmROW09? NFXtZ5JqdmS3Y3XzJIEhe2mpbnnmbYNidnRiaX7jdoVie2ViaX6geIhmKHC{b33veIVzKGGldHn2bZRq\XNib3[gSU1k[WRuwrDDSGgyNCCjbnVCpGNFUDN? NF7SNJozPjB4MUe0Oy=>
A549 NIPDUnlHfW6ldHnvckBCe3OjeR?= MUOyM|Uh|ryP NFfVN|AzPCCq NWLVSIVOTE2VTx?= NXmyXI9mcGG|IHGg[4Vv\XKjbDDFUXQhemW4ZYLzZYwh\W[oZXP0xsA> MV2yOlA3OTd2Nx?=
T24 NHn6NXBHfW6ldHnvckBCe3OjeR?= MXiyM|Uh|ryP MXSyOEBp NH6yfohFVVOR NYrLbXJHcGG|IHGg[4Vv\XKjbDDFUXQhemW4ZYLzZYwh\W[oZXP0xsA> NIjSOWkzPjB4MUe0Oy=>
Mia-Paca2 Mnm2SpVv[3Srb36gRZN{[Xl? M{PaflIwPSEQvF2= M{XD[VI1KGh? MWTEUXNQ NWrpN2d5cGG|IHGg[4Vv\XKjbDDFUXQhemW4ZYLzZYwh\W[oZXP0xsA> NGTmXoMzPjB4MUe0Oy=>
A549 M2HqSGZ2dmO2aX;uJGF{e2G7 NVH3blZYOC5yMfMAl|XDqM7:TR?= MYW3NkBp M{jyfmROW09? M4jZZYVvcGGwY3XzJHNRNURicILveIVqdiCneIDy[ZN{cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{IHH0JINwdmOnboTyZZRqd26|IH;mJJVxKHSxIEZCpO69VcLi M4ruV|I2QDR|MEC1
A549 MWPGeY5kfGmxbjDBd5NigQ>? NWfHeZJzPcLizszN MWKwMVEhcA>? NGLTUFhFVVOR M3;YV4lv[3KnYYPld{BCWC1zIHHjeIl3[XSrb36gJIFnfGW{IEOwJI1qdg>? NX3uXohSOjV6NEOwNFU>
Hep3B M4TSfGNmdGxiVnnhZoltcXS7IFHzd4F6 MY[wMVIxKM7:TR?= MXG0POKhcA>? NIjpcFRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MmrHNlQ3PTd|OUi=
HepG2 MkS1R4VtdCCYaXHibYxqfHliQYPzZZk> MlLINE0zOCEQvF2= NUj1VGRHPDkEoHi= MX;k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVjVVo1IOjR4NUezPVg>
PLC5 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXGwMVIxKM7:TR?= NFKwblQ1QMLiaB?= MUjk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MlHGNlQ3PTd|OUi=
HuH7 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUfyfJk{OC1{MDFOwG0> Mo\XOFjDqGh? MoXy[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NIPTdI4zPDZ3N{O5PC=>
SK-Hep1 NEXW[3hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVqwMVIxKM7:TR?= NGXt[WY1QMLiaB?= NH:4[Xhl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MVSyOFY2PzN7OB?=
Hep3B NUD4OGFZSXCxcITvd4l{KEG|c3H5 NGTp[JUxNTJyIN88US=> NYXNVHdEPDkEoHi= NE\ZVlFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHTvd4Uh\GWyZX7k[Y51dHl? Ml;sNlQ3PTd|OUi=
HepG2 M3q0OWFxd3C2b4Ppd{BCe3OjeR?= MmTmNE0zOCEQvF2= MWC0POKhcA>? M{nPNolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? MWmyOFY2PzN7OB?=
PLC5 NXi5SYVSSXCxcITvd4l{KEG|c3H5 MkDaNE0zOCEQvF2= Ml;DOFjDqGh? M2XiRolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? NYjIUpJNOjR4NUezPVg>
HuH7 MYPBdI9xfG:|aYOgRZN{[Xl? M13LZVAuOjBizszN M1TXN|Q5yqCq MkTKbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NVvBOIpxOjR4NUezPVg>
SK-Hep1 MnzsRZBweHSxc3nzJGF{e2G7 MXOwMVIxKM7:TR?= MoHIOFjDqGh? NXr0fIV5cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M4Lj[lI1PjV5M{m4
H1703 M4HydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zYPWlEPTB;MD6wOUDPxE1? NV;qPHlkOjN5Mkm0NFM>


Methods Test Index PMID
Western blot
Fibronectin / Collagen 1a1; 

PubMed: 26072676     

(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.

p-SMAD3 / SMAD3 / p-p38 MAPK / p38 MAPK ; 

PubMed: 26072676     

IMR-90 fibroblasts were serum starved overnight and cotreated with or without TGF-β1 (2.5 ng/ml) and increasing doses of nintedanib (0.5, 1, and 2 μM) for 1 hour. Expression of pS423/425-SMAD3, SMAD3, pT180/Y182-p38 mitogen-activated protein kinase (MAPK), and p38 MAPK was evaluated by Western blotting. 

Cyclin A / Cyclin D1 / Cyclin E / CDK2 / CDK4 / CDK6; 

PubMed: 29934570     

Western blot based detection of cell cycle associated molecules viz., Cyclins A, D1 and E, and CDKs 2, 4 and 6 in PC3 cells after 72 hours of Nintedanib treatment. 

p-EGFR / FGFR1 / p-AKT / AKT / p-ERK / ERK; 

PubMed: 27581340     

Effects of nintedanib on FGFR1, ERK, and AKT phosphorylation in FGFR1 CNG‐positive lung squamous cell carcinoma cell lines. H520 and LK‐2 cells were incubated for 6 h in the presence of the indicated concentrations of nintedanib, after which cell lysates (25 μg soluble protein) were subjected to immunoblot analysis with antibodies to the indicated proteins.

26072676 29934570 27581340
Vimentin / E-cadherin ; 

PubMed: 29934570     

Immunoflouresence staining for Vimentin (green) and E-cadherin (red) in DMSO control and 2.5 µM Nintedanib treated PC3 cells after 72 h of incubation. Representative flourescent pictures are shown at 600X. DAPI: 4′,6-diamidino-2-phenylindole.

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]


- 合併

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]
- 合併
  • 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.
- 合併
  • 動物モデル: FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 xenografts in Athymic NMRI-nu/nu female mice
  • 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
Smiles COC(=O)C1=CC=C\2C(=C1)NC(=O)C2=C(NC3=CC=C(C=C3)N(C)C(=O)CN4CCN(C)CC4)/C5=CC=CC=C5


投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
% DMSO % % Tween 80 % ddH2O





質量 (mg) = 濃度 (mM) x 体積 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03283007 Recruiting Drug: Nintedanib|Drug: Placebo Lung-transplant Recipients Assistance Publique - Hôpitaux de Paris October 30 2019 Phase 3
NCT03710824 Suspended Drug: Nintedanib Idiopathic Pulmonary Fibrosis Boehringer Ingelheim February 28 2019 --
NCT03958071 Active not recruiting Drug: Nintedanib|Drug: Pirfenidone|Other: Untreated Cohort Idiopathic Pulmonary Fibrosis Boehringer Ingelheim February 1 2019 --
NCT03725852 Active not recruiting Drug: GLPG1205|Drug: Placebo Idiopathic Pulmonary Fibrosis Galapagos NV September 27 2018 Phase 2
NCT03287947 Suspended Drug: nintedanib Appendix Cancer Jimmy Hwang|Boehringer Ingelheim|Atrium Health November 10 2017 Phase 2



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