Nintedanib (BIBF 1120)

Catalog No.S1010

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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Nintedanib (BIBF 1120) Chemical Structure

Nintedanib (BIBF 1120) Chemical Structure
Molecular Weight: 539.62

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Product Description

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.
Targets VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
LCK [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)

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IC50 13 nM 13 nM 16 nM 26 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SKOV3MVzGeY5kfGmxbjDBd5NigQ>?MlnrOUDDvU1?NU[5eXVFOjRiaB?=NVLaPYFWTE2VTx?=NXzQNXpxcW6mdXPld{BiKHOrZ37p[olk[W62IHnuZ5Jm[XOnIHnuJJRp\SCycn;tc5RmeiCjY4Tpeol1cWW|IH;mJGUu[2GmLNMgR2RJOSxiYX7kxsBETEh|MVqyOlA3OTd2Nx?=
A549MmjESpVv[3Srb36gRZN{[Xl?NF[2T4UzNzVizszNMX2yOEBpNUW0VYFRTE2VTx?=NH\uWoZp[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=>MYGyOlA3OTd2Nx?=
T24MVTGeY5kfGmxbjDBd5NigQ>?M4nKVlIwPSEQvF2=M3PqN|I1KGh?NY\aWHh{TE2VTx?=MnS0bIF{KGFiZ3Xu[ZJidCCHTWSgdoV3\XK|YXyg[YZn\WO2wrC=NV;KN45pOjZyNkG3OFc>
Mia-Paca2MmK1SpVv[3Srb36gRZN{[Xl?NVXIWHBtOi93IN88US=>M2rXT|I1KGh?NGn4RmZFVVORNEHtPFZp[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=>MV6yOlA3OTd2Nx?=
A549NHzTNZlHfW6ldHnvckBCe3OjeR?=NHLkd4ExNjBz4pETOeKh|ryPNHLLSnczPCCqM2fSR2ROW09?NHW3T3FqdmS3Y3XzJHNHXFCGwrDtVm5CKGW6cILld5Nqd25iZH;z[UBl\XCnbnTlcpRtgQ>?NF\qcZkzPTh2M{CwOS=>
A549NEfneJJHfW6ldHnvckBCe3OjeR?=NHnkbW4xNjBz4pETOeKh|ryPNFv1cog4OiCqNWDNNXVmTE2VTx?=NIPjTohmdmijbnPld{BUWC2GIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6ncjDheEBkd26lZX70doF1cW:wczDv[kB2eCC2bzC1xsDPxE4EoB?=NH3Meo8zPTh2M{CwOS=>
A549NI\EcnlHfW6ldHnvckBCe3OjeR?=NVS4boFbPcLizszNNGOyU4oxNTFiaB?=NXf5[|hmTE2VTx?=NV;NUYc2cW6lcnXhd4V{KEGSLUGgZYN1cX[jdHnvckAh[W[2ZYKgN|AhdWmwM3fnNFI2QDR|MEC1
Hep3BM2XRcmNmdGxiVnnhZoltcXS7IFHzd4F6MmryNE0zOCEQvF2=NVG4O|E5PDkEoHi=MonJ[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?NW[zPHljOjR4NUezPVg>
HepG2MkH4R4VtdCCYaXHibYxqfHliQYPzZZk>MnzaNE0zOCEQvF2=Mk\zOFjDqGh?NFr4U49l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=NEC5d5QzPDZ3N{O5PC=>
PLC5M4n3UGNmdGxiVnnhZoltcXS7IFHzd4F6MXewMVIxKM7:TR?=NH[2fIc1QMLiaB?=NUHa[XF6\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm=NVXZTnpWOjR4NUezPVg>
HuH7MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=>NVnpUXRIOC1{MDFOwG0>NX3tb5hmPDkEoHi=NW\BSHFU\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm=NX3EZ3BEOjR4NUezPVg>
SK-Hep1Ml\4R4VtdCCYaXHibYxqfHliQYPzZZk>MUKwMVIxKM7:TR?=NX6wdldiPDkEoHi=MULk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?M{HqbVI1PjV5M{m4
Hep3BMYfBdI9xfG:|aYOgRZN{[Xl?NFT4S5MxNTJyIN88US=>MX:0POKhcA>?NXiwPW1DcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7MWOyOFY2PzN7OB?=
HepG2NYHYdW1vSXCxcITvd4l{KEG|c3H5M1O1cFAuOjBizszNM{Pve|Q5yqCqM4PDcolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>?NYXtUo4{OjR4NUezPVg>
PLC5MkO1RZBweHSxc3nzJGF{e2G7NWjWUm5wOC1{MDFOwG0>MnL4OFjDqGh?M2Tucolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>?M{\YelI1PjV5M{m4
HuH7M4PWNWFxd3C2b4Ppd{BCe3OjeR?=NWLPN3VqOC1{MDFOwG0>M4PBcFQ5yqCqMoflbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6NGrtT3EzPDZ3N{O5PC=>
SK-Hep1M1fnUmFxd3C2b4Ppd{BCe3OjeR?=NFrQbIYxNTJyIN88US=>NW\L[nV[PDkEoHi=MXHpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk>NXi3RnE{OjR4NUezPVg>
H1703NFexNI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1jDe2lEPTB;MD6wOUDPxE1?MVKyN|czQTRyMx?=

... 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]
Features

Protocol(Only for Reference)

Kinase Assay: [3]

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 Assay: [1]

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.

Animal Study: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Hilberg F, et al. Cancer Res, 2008, 68(12), 4774-4782.

[2] Frank H, et al. J Thorac Oncol, 2007, 2(8), S380. doi: 10.1097/01.JTO.0000283231.76336.01

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02808247 Not yet recruiting Sarcoma, Soft Tissue European Organisation for Research and Treatment of Cance  ...more European Organisation for Research and Treatment of Cancer - EORTC|Boehringer Ingelheim January 2017 Phase 2
NCT02730416 Not yet recruiting Endometrial Cancer Nordic Society for Gynaecologic Oncology|North Eastern Ge  ...more Nordic Society for Gynaecologic Oncology|North Eastern Germany Society of Gynaecologic Oncology|Belgian Gynaecological Oncology Group|ARCAGY/ GINECO GROUP July 2016 Phase 2
NCT02780700 Recruiting Colorectal Neoplasms Boehringer Ingelheim July 2016 Phase 2
NCT02665143 Recruiting Relapsed/Refractory Acute Myeloid Leukemia Yale University|Vanderbilt University June 2016 Phase 1|Phase 2
NCT02788474 Recruiting Idiopathic Pulmonary Fibrosis Boehringer Ingelheim June 2016 Phase 4

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Chemical Information

Download Nintedanib (BIBF 1120) SDF
Molecular Weight (MW) 539.62
Formula

C31H33N5O4

CAS No. 656247-17-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms Intedanib
Solubility (25°C) * In vitro DMSO 6 mg/mL (11.11 mM)
Ethanol 3 mg/mL (5.55 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name (Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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