Nintedanib (BIBF 1120)

Catalog No.S1010 Synonyms: Intedanib, Vargatef, Ofev

For research use only.

Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 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.

Nintedanib (BIBF 1120) Chemical Structure

CAS No. 656247-17-5

Selleck's Nintedanib (BIBF 1120) has been cited by 109 publications

Purity & Quality Control

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Biological Activity

Description Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 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)
VEGFR1 [1]
(Cell-free assay)
Click to View More Targets
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 NFPLPYlHfW6ldHnvckBCe3OjeR?= MmfHOUDDvU1? M{PxRVI1KGh? NHHlc3pFVVOR NX[4d2trcW6mdXPld{BiKHOrZ37p[olk[W62IHnuZ5Jm[XOnIHnuJJRp\SCycn;tc5RmeiCjY4Tpeol1cWW|IH;mJGUu[2GmLNMgR2RJOSxiYX7kxsBETEh| Mn\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNkG3OFcoRjJ4ME[xO|Q4RC:jPh?=
A549 MVLGeY5kfGmxbjDBd5NigQ>? M1vqbFIwPSEQvF2= M2ewR|I1KGh? NXrzS3g1TE2VTx?= NIS1XY9p[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=> NE[weFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC2NVc1Pyd-Mk[wOlE4PDd:L3G+
T24 M3rxSWZ2dmO2aX;uJGF{e2G7 M3n1cVIwPSEQvF2= M3vROVI1KGh? MYjEUXNQ M2LFb4hieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg NWnHT5ZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOlE4PDdpPkK2NFYyPzR5PD;hQi=>
Mia-Paca2 NHTNXW5HfW6ldHnvckBCe3OjeR?= MUeyM|Uh|ryP NYPqSpNHOjRiaB?= NFTBeJZFVVOR NHXtXmxp[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=> Mle4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNkG3OFcoRjJ4ME[xO|Q4RC:jPh?=
A549 MlT5SpVv[3Srb36gRZN{[Xl? NXjSNXh[OC5yMfMAl|XDqM7:TR?= NVvLTmdiOjRiaB?= MVTEUXNQ MX7pcoR2[2W|IGPGWHBFyqCvUl7BJIV5eHKnc4Ppc44h\G:|ZTDk[ZBmdmSnboTsfS=> NH\NbYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi0N|AxPSd-MkW4OFMxODV:L3G+
A549 M3LFfWZ2dmO2aX;uJGF{e2G7 MYewMlAy6oDVNdMg{txO MkXTO|IhcA>? NWnC[45DTE2VTx?= MWTlcohidmOnczDTVE1FKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meiCjdDDjc45k\W62cnH0bY9veyCxZjD1dEB1dyB3wrFOwG3DqA>? NWLBbZhGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OFMxODVpPkK1PFQ{ODB3PD;hQi=>
A549 MnzmSpVv[3Srb36gRZN{[Xl? NI\SNGc2yqEQvF2= MYmwMVEhcA>? MYDEUXNQ NIf5cmlqdmO{ZXHz[ZMhSVBvMTDhZ5RqfmG2aX;uJEBi\nSncjCzNEBucW5? NYLIbVhzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OFMxODVpPkK1PFQ{ODB3PD;hQi=>
Hep3B NGTDOFlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEWwVXYxNTJyIN88US=> Ml;6OFjDqGh? NWHtbGp4\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NWrWVYkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HepG2 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEDifYgxNTJyIN88US=> M{DtdVQ5yqCq M1r3VYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
PLC5 M2T3emNmdGxiVnnhZoltcXS7IFHzd4F6 NWPEd2dmOC1{MDFOwG0> NYPrVYt7PDkEoHi= M33wUYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
HuH7 NFHtRWZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFL1N5MxNTJyIN88US=> MYm0POKhcA>? MmDC[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NGTud|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
SK-Hep1 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYKwMVIxKM7:TR?= MoP3OFjDqGh? NEjYdpZl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MkSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N|k5RC:jPh?=
Hep3B NIjmeWRCeG:ydH;zbZMhSXO|YYm= MVGwMVIxKM7:TR?= NITBOpM1QMLiaB?= MUDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> NY\DSHE1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HepG2 MUTBdI9xfG:|aYOgRZN{[Xl? M1izeVAuOjBizszN MVe0POKhcA>? Ml3mbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
PLC5 NEDEUpNCeG:ydH;zbZMhSXO|YYm= NHrN[G4xNTJyIN88US=> MX20POKhcA>? MkLObY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NVHhN2FLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HuH7 MYnBdI9xfG:|aYOgRZN{[Xl? NWnRSlRnOC1{MDFOwG0> M1LzcFQ5yqCq M1LxZYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? NILJcGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
SK-Hep1 MYTBdI9xfG:|aYOgRZN{[Xl? MUGwMVIxKM7:TR?= MnTaOFjDqGh? Mnu4bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NIj4RnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
H1703 NHrvdW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTreIU3UUN3ME2wMlA2KM7:TR?= Ml32QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFMoRjJ|N{K5OFA{RC:jPh?=
Sf9 MoLySpVv[3Srb36gZZN{[Xl? MVWyNEBucW6| MmXkTY5pcWKrdHnvckBw\iCvb4Xz[UBIW1RvZoXz[YQhXkWJRmKyJIV5eHKnc4Pl[EBqdiCVZkmgbY5{\WO2IHPlcIx{KGGodHXyJFIxKG2rboOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OCB;IECuNFE{KM7:TT6= M{PqfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NUW5OVI1Lz5zOEW1PVUzPDxxYU6=
Sf9 MnrpSpVv[3Srb36gZZN{[Xl? NG\5SlYzOCCvaX7z NVTofFRmUW6qaXLpeIlwdiCxZjDoeY1idiCJU2St[pV{\WRiVlXHSnIzKGW6cILld5Nm\CCrbjDT[lkhcW6|ZXP0JINmdGy|IHHmeIVzKDJyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvODJzIN88UU4> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDV3OUWyOEc,OTh3NUm1NlQ9N2F-
NIH3T3 M3;RPWZ2dmO2aX;uJIF{e2G7 M{TOeVUxKG6P Ml\nNUBpeg>? MmG5TY5pcWKrdHnvckBw\iCYRVfGVlIhfHKjboPm[YN1\WRiaX6gcY92e2ViTlnIN3Q{KGOnbHzzJIF1KDVyIH7NJIlv[3WkYYTl[EBnd3JiMTDodkBu\WG|dYLl[EBi\nSncjCzNkBpenNid3HzbI92fCCob3zsc5dm\CCkeTDWSWdHKHO2aX31cIF1cW:wIH\vdkAyOCCvaX7zJIJ6KFenc4Tldo4h[myxdITpcoc> NF65T2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEW1PVUzPCd-MUi1OVk2OjR:L3G+
HT-29 Ml3QRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2jTTVczKGi{cx?= NWjIfYJ{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOE46KM7:TT6= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF7ME[1Nkc,OjhzOUC2OVI9N2F-
SKOV3 MofxRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NUn5blVlPzJiaILz MoTkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMkiuO|Yh|ryPLh?= NILCXlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG5NFY2Oid-MkixPVA3PTJ:L3G+
BL21 (DE3) MYHGeY5kfGmxbjDhd5NigQ>? MV6zNEBucW6| M2DRW2lvcGmkaYTpc44hd2ZiSHnzOk11[WepZXSgUWVNUyClYYThcJl1cWNiZH;tZYlvKChzIITvJFM1OCC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gSZNkcGW{aXPobYEh[2:uaTDCUFIyKCiGRUOpJINmdGy|IIXzbY5oKEKlbD3HUEBieyC|dXLzeJJifGVibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BqdiCycnXz[Y5k\SCxZjDb[4FudWF|MmDdRXRRKGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7nJI1mfGixZDygT4khRSByLkCwOVYh|ryPLh?= NYfTUHdyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizOVE3ODdpPkK4N|UyPjB5PD;hQi=>
BL21 (DE3) NGTpUYdHfW6ldHnvckBie3OjeR?= NXLHXYFtOzBibXnudy=> NEHLTIFKdmirYnn0bY9vKG:oIFjpd|YufGGpZ3XkJG1GVEtiY3H0ZYx6fGmlIHTvcYFqdiBqMTD0c{A{PDBicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGV{[2incnnjbIliKGOxbHmgRmwzOSBqRFWzLUBk\WyuczD1d4lv\yCEY3ytS2wh[XNic4Xid5Rz[XSnIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMhcW5icILld4Vv[2Vib3[gX4didW2jM{LQYWFVWCCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[{Bu\XSqb3SsJGlEPTBiPTCwMlA1OyEQvF2u NF\XV2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO1NVYxPyd-MkizOVE3ODd:L3G+
HT-29 MX\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXS3NkBpenN? MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkizJO69VS5? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh{NkC4OEc,Ojh6Mk[wPFQ9N2F-
MCF7 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIDkcJc4OiCqcoO= M4jVVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iOD6yPEDPxE1w MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh{NkC4OEc,Ojh6Mk[wPFQ9N2F-
A549 MXzBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1TqUlczKGi{cx?= NEXNb3RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEKyMlYzKM7:TT6= NVPVOWo5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4NlYxQDRpPkK4PFI3ODh2PD;hQi=>
NIH/3T3 M4n6eGZ2dmO2aX;uJIF{e2G7 MXK0NkBpenN? M4D1UWlvcGmkaYTpc44hd2ZiUFTHSnIhcW5ibX;1d4UhVkmKL{PUN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icnXjc41jcW6jboSgbJVu[W5iUFTHSk1DSi2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA1OiCqcoOgZpkh[2WubDD0bZRmeiB7NjDhdZVmd3W|IH;u[UB{d2y3dHnvckBj[XOnZDDhd5NigSxiSVO1NEA:KDBwMEi1JO69VS5? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF3MkC0OUc,OjlzNUKwOFU9N2F-
Sf9 NHf1XZBHfW6ldHnvckBie3OjeR?= NWrzXoV2UW6qaXLpeIlwdiCxZjDoeY1idiCYRVfGVlIh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OCB;IECuNFA2KM7:TT6= M3\jfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUKyOFY2Lz5zOUWyNlQ3PTxxYU6=
NIH3T3 NVXuXm9uTnWwY4Tpc44h[XO|YYm= NHvpc3UyKGi{ MVLJcohq[mm2aX;uJI9nKF[HR1[td5RqdXWuYYTl[EBpfW2jbjDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKGW6cILld5Nm\CCrbjDtc5V{\SCQSVizWFMh[2WubIOgdJJmfHKnYYTl[EBnd3JiMTDodkBu\WG|dYLl[EA{OiCqcoOgZYZ1\XJiZIL1[{Bld3OnIHL5JIludXWwb4Dy[YNqeGm2YYTpc44h[mG|ZXSgdJVte2VvY3jhd4Uh\XiyZYLpcYVvfA>? M2PnT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUKyOFY2Lz5zOUWyNlQ3PTxxYU6=
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SK-N-SH MW\xTHRUKGG|c3H5 M4TMUpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz M4rrW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 Mo\KdWhVWyCjc4PhfS=> NGfvRndyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz NFX6ZW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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LAN-5 MYjxTHRUKGG|c3H5 MVrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDMRW4uPSClZXzsdy=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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MG 63 (6-TG R) MYnxTHRUKGG|c3H5 MVTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NVfNSnBYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh30 NUW1RVdseUiWUzDhd5NigQ>? M1rLZpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOzBiY3XscJM> M2fRNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS NGD3UXVyUFSVIHHzd4F6 NHvSeVFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBWNTJiT2OgZ4VtdHN? NEDzbWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 MnzCdWhVWyCjc4PhfS=> MmD1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgU2hUNTVyIHPlcIx{ M2HsXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MkXqdWhVWyCjc4PhfS=> NF3OV2pyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{ MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 M1HZTpFJXFNiYYPzZZk> NU\OWlBneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> M2r3cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 M{fOWJFJXFNiYYPzZZk> NHvC[lZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NIi3[2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 NF7LbZVyUFSVIHHzd4F6 NXv0W3BDeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz M3nSdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 M37xT5FJXFNiYYPzZZk> M{nTUZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG5DOTZ2MzDj[Yxtew>? NYrlOpU4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NIDlXGtyUFSVIHHzd4F6 NUXKOmFOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MnruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 MlvtdWhVWyCjc4PhfS=> MorKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=> MkLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 NXjwTmJieUiWUzDhd5NigQ>? MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFE5KGOnbHzz M{PSZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Assay
Methods Test Index PMID
Western blot Fibronectin / Collagen 1a1 ; p-SMAD3 / SMAD3 / p-p38 MAPK / p38 MAPK ; Cyclin A / Cyclin D1 / Cyclin E / CDK2 / CDK4 / CDK6 ; p-EGFR / FGFR1 / p-AKT / AKT / p-ERK / ERK 26072676 29934570 27581340
Immunofluorescence Vimentin / E-cadherin 29934570
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]

Protocol (from 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 Research:[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 Research:[1]
  • Animal Models: FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 xenografts in Athymic NMRI-nu/nu female mice
  • Dosages: 100 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

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.

0.25mg/mL

Chemical Information

Molecular Weight 539.62
Formula

C31H33N5O4

CAS No. 656247-17-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)OC)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04976036 Recruiting Drug: Nintedanib|Drug: Placebo Telangiectasia Hereditary Hemorrhagic Dr. Romain Lazor|Boehringer Ingelheim|Centre Hospitalier Universitaire Vaudois May 5 2022 Phase 2
NCT04971746 Completed Drug: Pirfenidone|Drug: GLPG4716|Drug: Nintedanib Healthy Galapagos NV July 19 2021 Phase 1
NCT04888715 Completed Drug: DWN12088|Drug: Pirfenidone|Drug: Nintedanib Idiopathic Pulmonary Fibrosis Daewoong Pharmaceutical Co. LTD. July 23 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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