Nintedanib (BIBF 1120)

Catalog No.S1010 Synonyms: Intedanib

Nintedanib (BIBF 1120) Chemical Structure

Molecular Weight(MW): 539.62

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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In DMSO USD 240 In stock
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8 Customer Reviews

  • 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.

Purity & Quality Control

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Biological Activity

Description 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
In vitro

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 MUTGeY5kfGmxbjDBd5NigQ>? MVS1JOK2VQ>? M1;GXlI1KGh? MkPKSG1UVw>? NVjuXnp4cW6mdXPld{BiKHOrZ37p[olk[W62IHnuZ5Jm[XOnIHnuJJRp\SCycn;tc5RmeiCjY4Tpeol1cWW|IH;mJGUu[2GmLNMgR2RJOSxiYX7kxsBETEh| NH3tOXYzPjB4MUe0Oy=>
T24 M3fjb2Z2dmO2aX;uJGF{e2G7 Mo\qNk82KM7:TR?= NV\ne2hnOjRiaB?= MV7EUXNQ NV7vSVF4cGG|IHGg[4Vv\XKjbDDFUXQhemW4ZYLzZYwh\W[oZXP0xsA> M3K3fFI3ODZzN{S3
Mia-Paca2 NI\ibpZHfW6ldHnvckBCe3OjeR?= MX2yM|Uh|ryP MVKyOEBp NFPsN5VFVVOR M1v0cYhieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg MUmyOlA3OTd2Nx?=
A549 M2TxdGZ2dmO2aX;uJGF{e2G7 MYWwMlAy6oDVNdMg{txO Mm\HO|IhcA>? NIqzRXlFVVOR NFXnOZhmdmijbnPld{BUWC2GIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6ncjDheEBkd26lZX70doF1cW:wczDv[kB2eCC2bzC1xsDPxE4EoB?= MVeyOVg1OzByNR?=
A549 MnjSSpVv[3Srb36gRZN{[Xl? MkHyOeKh|ryP NY\vZ|FjOC1zIHi= NYWwNIRYTE2VTx?= MknobY5kemWjc3XzJGFRNTFiYXP0bZZifGmxbjCgZYZ1\XJiM{CgcYlv NXTDTGhVOjV6NEOwNFU>
Hep3B NEPaXVJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlzTNE0zOCEQvF2= MnfGOFjDqGh? NYrRTpQ{\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= M2rnXFI1PjV5M{m4
HepG2 M2j5[GNmdGxiVnnhZoltcXS7IFHzd4F6 NVvHcWdUOC1{MDFOwG0> MmSxOFjDqGh? NGTvdFBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWCwV4hlOjR4NUezPVg>
PLC5 M3f6TWNmdGxiVnnhZoltcXS7IFHzd4F6 MWiwMVIxKM7:TR?= MkXpOFjDqGh? MUTk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M2TYU|I1PjV5M{m4
HuH7 Ml;YR4VtdCCYaXHibYxqfHliQYPzZZk> NWjscXp6OC1{MDFOwG0> NFP0Vnk1QMLiaB?= NHPi[oJl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MVWyOFY2PzN7OB?=
SK-Hep1 NFTqcXhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkOzNE0zOCEQvF2= NVP5UWZMPDkEoHi= MXnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MV[yOFY2PzN7OB?=
Hep3B NFzicIpCeG:ydH;zbZMhSXO|YYm= M2PhblAuOjBizszN MnXkOFjDqGh? M3:5dYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? Mo\WNlQ3PTd|OUi=
HepG2 MlrERZBweHSxc3nzJGF{e2G7 NFLuSFUxNTJyIN88US=> MYO0POKhcA>? NUXPdIZvcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NIXNXHAzPDZ3N{O5PC=>
PLC5 NELlcI9CeG:ydH;zbZMhSXO|YYm= M1PHWFAuOjBizszN NXH1RmNrPDkEoHi= M4jTPIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? MV6yOFY2PzN7OB?=
HuH7 NGe3TGlCeG:ydH;zbZMhSXO|YYm= MmLMNE0zOCEQvF2= Mn3TOFjDqGh? MXPpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> M2nJ[VI1PjV5M{m4
SK-Hep1 MormRZBweHSxc3nzJGF{e2G7 NUTSOm9ROC1{MDFOwG0> M3nyVlQ5yqCq MnL2bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NFnOSXczPDZ3N{O5PC=>
H1703 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf0OppKSzVyPUCuNFUh|ryP Ml3KNlM4Ojl2MEO=

... Click to View More Cell Line Experimental Data

In vivo 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]


Kinase Assay:[3]
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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.
Cell Research:[1]
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  • Cell lines: HUVEC, HUASMC, and BRP cell lines
  • Concentrations: 50 nM
  • Incubation Time: 2 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 xenografts in Athymic NMRI-nu/nu female mice
  • Formulation: In a 0.5 % Natrosol solution
  • Dosages: 100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 6 mg/mL (11.11 mM)
Ethanol 3 mg/mL (5.55 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 539.62


CAS No. 656247-17-5
Storage powder
in solvent
Synonyms Intedanib

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03710824 Not yet recruiting Idiopathic Pulmonary Fibrosis Boehringer Ingelheim December 14 2018 --
NCT03675581 Recruiting Scleroderma Systemic Boehringer Ingelheim November 8 2018 Phase 1
NCT03717012 Not yet recruiting Idiopathic Pulmonary Fibrosis Boehringer Ingelheim November 15 2018 Phase 4
NCT03562416 Not yet recruiting Idiopathic Pulmonary Fibrosis|Lung Transplant; Complications Temple University|Boehringer Ingelheim October 2018 Phase 2
NCT03283007 Not yet recruiting Lung-transplant Recipients Assistance Publique - Hôpitaux de Paris October 2018 Phase 3
NCT03513484 Not yet recruiting Acute Myeloid Leukemia With t(9;11)(p22.3;q23.3); MLLT3-KMT2A|Fibroblast Growth Factor Basic Form Measurement|FLT3 Internal Tandem Duplication|Recurrent Adult Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia Northwestern University|Robert H. Lurie Cancer Center|Boehringer Ingelheim|National Cancer Institute (NCI) September 30 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID