Nintedanib (BIBF 1120)

For research use only.

Catalog No.S1010 Synonyms: Intedanib, Vargatef, Ofev

98 publications

Nintedanib (BIBF 1120) Chemical Structure

CAS No. 656247-17-5

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.

Selleck's Nintedanib (BIBF 1120) has been cited by 98 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

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)
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 MVrGeY5kfGmxbjDBd5NigQ>? NIrKcpc2KML3TR?= NVzWdoJtOjRiaB?= MoHvSG1UVw>? NW\V[GN6cW6mdXPld{BiKHOrZ37p[olk[W62IHnuZ5Jm[XOnIHnuJJRp\SCycn;tc5RmeiCjY4Tpeol1cWW|IH;mJGUu[2GmLNMgR2RJOSxiYX7kxsBETEh| NXHGXItQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOlE4PDdpPkK2NFYyPzR5PD;hQi=>
A549 MmrISpVv[3Srb36gRZN{[Xl? M{ntN|IwPSEQvF2= M4ftUVI1KGh? MnS1SG1UVw>? MUjoZZMh[SCpZX7ldoFtKEWPVDDy[ZZmenOjbDDl[oZm[3UEoB?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB4MUe0O{c,OjZyNkG3OFc9N2F-
T24 M1va[2Z2dmO2aX;uJGF{e2G7 NXLURWxIOi93IN88US=> MmXmNlQhcA>? MWLEUXNQ NVvCZYhucGG|IHGg[4Vv\XKjbDDFUXQhemW4ZYLzZYwh\W[oZXP0xsA> MnzqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNkG3OFcoRjJ4ME[xO|Q4RC:jPh?=
Mia-Paca2 NITkdVNHfW6ldHnvckBCe3OjeR?= Mm\yNk82KM7:TR?= NF:zXJgzPCCq M2HvOGROW09? MUnoZZMh[SCpZX7ldoFtKEWPVDDy[ZZmenOjbDDl[oZm[3UEoB?= Mmr3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNkG3OFcoRjJ4ME[xO|Q4RC:jPh?=
A549 MoPVSpVv[3Srb36gRZN{[Xl? Mk[4NE4xOeLCk{ZCpO69VQ>? NUnkfoE4OjRiaB?= M1i2NmROW09? MnfNbY5lfWOnczDTSnRRTMLibWLORUBmgHC{ZYPzbY9vKGSxc3Wg[IVx\W6mZX70cJk> NHXkV2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi0N|AxPSd-MkW4OFMxODV:L3G+
A549 MVrGeY5kfGmxbjDBd5NigQ>? MUGwMlAy6oDVNdMg{txO NG\wbVQ4OiCq M4D6Z2ROW09? MUnlcohidmOnczDTVE1FKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meiCjdDDjc45k\W62cnH0bY9veyCxZjD1dEB1dyB3wrFOwG3DqA>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh2M{CwOUc,OjV6NEOwNFU9N2F-
A549 M1:1SGZ2dmO2aX;uJGF{e2G7 NHO5Rlk2yqEQvF2= NEf2WXMxNTFiaB?= M2PCe2ROW09? NVK3O4FJcW6lcnXhd4V{KEGSLUGgZYN1cX[jdHnvckAh[W[2ZYKgN|AhdWmw NYPySZpzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OFMxODVpPkK1PFQ{ODB3PD;hQi=>
Hep3B MmHyR4VtdCCYaXHibYxqfHliQYPzZZk> NV;JVYpmOC1{MDFOwG0> M3LCRVQ5yqCq M3nPOoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MkfHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N|k5RC:jPh?=
HepG2 M3XmVmNmdGxiVnnhZoltcXS7IFHzd4F6 NVLJZ2w3OC1{MDFOwG0> NIr6eok1QMLiaB?= NGTnSZpl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYDsVnpoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
PLC5 NIPt[HZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnXnNE0zOCEQvF2= NILve3k1QMLiaB?= MXTk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NWL2boJvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HuH7 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFXoRnUxNTJyIN88US=> MnLnOFjDqGh? M3y1[YRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NYn1eGJ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
SK-Hep1 NFexZ2lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVewMVIxKM7:TR?= M2fNZlQ5yqCq MYDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
Hep3B NHXIO5pCeG:ydH;zbZMhSXO|YYm= NITKd3MxNTJyIN88US=> M123XVQ5yqCq MWHpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> NXfmU5BYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HepG2 Mn[yRZBweHSxc3nzJGF{e2G7 Mn;vNE0zOCEQvF2= NWPMdXpbPDkEoHi= NX\uepA4cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NH;VWZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
PLC5 NXXrToxFSXCxcITvd4l{KEG|c3H5 MUiwMVIxKM7:TR?= MWe0POKhcA>? MYXpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> NUjDNnhQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HuH7 MYXBdI9xfG:|aYOgRZN{[Xl? Mlq1NE0zOCEQvF2= M{DS[VQ5yqCq MlrVbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NVnkVndbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
SK-Hep1 NXLuVWxYSXCxcITvd4l{KEG|c3H5 M3nqdVAuOjBizszN NH63U2Y1QMLiaB?= NVixSYxtcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N|k5RC:jPh?=
H1703 NHPvbmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[wb2QzUUN3ME2wMlA2KM7:TR?= MoD6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFMoRjJ|N{K5OFA{RC:jPh?=
Sf9 MXHGeY5kfGmxbjDhd5NigQ>? Ml30NlAhdWmwcx?= NVj1Zox{UW6qaXLpeIlwdiCxZjDtc5V{\SCJU2St[pV{\WRiVlXHSnIzKGW6cILld5Nm\CCrbjDT[lkhcW6|ZXP0JINmdGy|IHHmeIVzKDJyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvODF|IN88UU4> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDV3OUWyOEc,OTh3NUm1NlQ9N2F-
Sf9 MkTGSpVv[3Srb36gZZN{[Xl? MV:yNEBucW6| M1yzUmlvcGmkaYTpc44hd2ZiaIXtZY4hT1OWLX\1d4VlKF[HR1\SNkBmgHC{ZYPz[YQhcW5iU3[5JIlve2WldDDj[YxteyCjZoTldkAzOCCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTBiPTCwMlAzOSEQvF2u MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDV3OUWyOEc,OTh3NUm1NlQ9N2F-
NIH3T3 MYTGeY5kfGmxbjDhd5NigQ>? MVi1NEBvVQ>? M2fSRlEhcHJ? MWPJcohq[mm2aX;uJI9nKF[HR1\SNkB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCQSVizWFMh[2WubIOgZZQhPTBibl2gbY5kfWKjdHXkJIZweiBzIHjyJI1m[XO3cnXkJIFnfGW{IEOyJIhzeyC5YYPoc5V1KG[xbHzve4VlKGK7IG\FS2Yhe3SrbYXsZZRqd25iZn;yJFExKG2rboOgZpkhX2W|dHXyckBjdG:2dHnu[y=> MoLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh3NUm1NlQoRjF6NUW5OVI1RC:jPh?=
HT-29 NEPZToJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFHyOmM4OiCqcoO= MlfuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iND65JO69VS5? M{LiZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUmwOlUzLz5{OEG5NFY2OjxxYU6=
SKOV3 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYG5b|ZSPzJiaILz MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB{OD63OkDPxE1w MnX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzOUC2OVIoRjJ6MUmwOlUzRC:jPh?=
BL21 (DE3) NHqwVZFHfW6ldHnvckBie3OjeR?= M2\LO|MxKG2rboO= MYDJcohq[mm2aX;uJI9nKEirc{[teIFo\2WmIF3FUGsh[2G2YXz5eIlkKGSxbXHpckApOSC2bzCzOFAhemW|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFXzZ4hmemmlaHnhJINwdGliQlyyNUApTEV|KTDj[YxteyC3c3nu[{BD[2xvR1ygZZMhe3Wkc4TyZZRmKG2nYYP1doVlKGGodHXyJFMxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiW3fhcY1iOzKSXVHUVEBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFvpJF0hOC5yMEW2JO69VS5? M3rJelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{WxOlA4Lz5{OEO1NVYxPzxxYU6=
BL21 (DE3) M2XWe2Z2dmO2aX;uJIF{e2G7 MWCzNEBucW6| NV\uO|VvUW6qaXLpeIlwdiCxZjDIbZM3NXSjZ3fl[EBOTUyNIHPheIFtgXSrYzDkc41icW5iKEGgeI8hOzRyIILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJGJNOjFiKFTFN{kh[2WubIOgeZNqdmdiQnPsMWdNKGG|IIP1ZpN1emG2ZTDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGmwIIDy[ZNmdmOnIH;mJHto[W2vYUOyVH1CXFBiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcochdWW2aH;kMEBKSzVyIE2gNE4xPDNizszNMi=> MkDuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|NUG2NFcoRjJ6M{WxOlA4RC:jPh?=
HT-29 NWjkS4ZkSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MXi3NkBpenN? Ml\KRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD64N{DPxE1w NFroU4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEiyOlA5PCd-Mki4NlYxQDR:L3G+
MCF7 NXX6UIZISW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NWPxfIQ5PzJiaILz M3r1XGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iOD6yPEDPxE1w Mor2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6Mk[wPFQoRjJ6OEK2NFg1RC:jPh?=
A549 MkKwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NVnvN5EyPzJiaILz NETpPFhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEKyMlYzKM7:TT6= MkjOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6Mk[wPFQoRjJ6OEK2NFg1RC:jPh?=
NIH/3T3 MVvGeY5kfGmxbjDhd5NigQ>? NY\yb|ZvPDJiaILz MYDJcohq[mm2aX;uJI9nKFCGR1\SJIlvKG2xdYPlJG5KUC9|VEOgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHKnY3;tZolv[W62IHj1cYFvKFCGR1[tRmIucW6mdXPl[EBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOFIhcHK|IHL5JINmdGxidHn0[ZIhQTZiYYH1[Y92eyCxbnWgd49tfXSrb36gZoF{\WRiYYPzZZktKEmFNUCgQUAxNjB6NTFOwG0v M3XBNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUWyNFQ2Lz5{OUG1NlA1PTxxYU6=
Sf9 MnfsSpVv[3Srb36gZZN{[Xl? MXPJcohq[mm2aX;uJI9nKGi3bXHuJHZGT0[UMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwJF0hOC5yMEWg{txONg>? NHnoTpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUWyNlQ3PSd-MUm1NlI1PjV:L3G+
NIH3T3 M{n1cmZ2dmO2aX;uJIF{e2G7 MoTmNUBpeg>? MV7Jcohq[mm2aX;uJI9nKF[HR1[td5RqdXWuYYTl[EBpfW2jbjDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKGW6cILld5Nm\CCrbjDtc5V{\SCQSVizWFMh[2WubIOgdJJmfHKnYYTl[EBnd3JiMTDodkBu\WG|dYLl[EA{OiCqcoOgZYZ1\XJiZIL1[{Bld3OnIHL5JIludXWwb4Dy[YNqeGm2YYTpc44h[mG|ZXSgdJVte2VvY3jhd4Uh\XiyZYLpcYVvfA>? NVPHWll7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1NlI1PjVpPkG5OVIzPDZ3PD;hQi=>
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NB1643 MoXJdWhVWyCjc4PhfS=> M2P2NZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG5DOTZ2MzDj[Yxtew>? M3u5bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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TC32 MmS3dWhVWyCjc4PhfS=> M32wTpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> Moj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 MXzxTHRUKGG|c3H5 MkPwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVogyQCClZXzsdy=> NEPCNY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay
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
Immunofluorescence
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.

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

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]
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  • 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.
    (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.
0.25mg/mL

* 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
Formula

C31H33N5O4

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

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04976036 Not yet recruiting Drug: Nintedanib|Drug: Placebo Telangiectasia Hereditary Hemorrhagic Dr. Romain Lazor|Boehringer Ingelheim|Centre Hospitalier Universitaire Vaudois September 2021 Phase 2
NCT04971746 Recruiting Drug: Pirfenidone|Drug: GLPG4716|Drug: Nintedanib Healthy Galapagos NV July 19 2021 Phase 1
NCT04888715 Recruiting Drug: DWN12088|Drug: Pirfenidone|Drug: Nintedanib Idiopathic Pulmonary Fibrosis Daewoong Pharmaceutical Co. LTD. July 23 2021 Phase 1
NCT04856111 Recruiting Drug: Pirfenidone|Drug: Nintedanib Novel Coronavirus-induced Lung Fibrosis Postgraduate Institute of Medical Education and Research March 17 2021 Phase 4
NCT04525547 Recruiting Drug: Nintedanib Idiopathic Pulmonary Fibrosis Boehringer Ingelheim January 13 2021 --

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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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID