Nintedanib (BIBF 1120)

For research use only. Not for use in humans.

製品コードS1010 別名:Intedanib, Vargatef, Ofev

Nintedanib (BIBF 1120)化学構造

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.

サイズ 価格(税別)  
10mM (1mL in DMSO) JPY 41800
JPY 21900
JPY 113200
JPY 212800
最寄りの販売代理店を探す

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください:[email protected]

バルク問合せ

文献中Selleckの製品使用例(89)

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV3 NF;KZoNHfW6ldHnvckBCe3OjeR?= Ml7kOUDDvU1? NY\wR2pSOjRiaB?= NFPxTJBFVVOR MlHBbY5lfWOnczDhJJNq\26rZnnjZY51KGmwY4LlZZNmKGmwIITo[UBxem:vb4TldkBi[3Srdnn0bYV{KG:oIFWtZ4FlNMLiQ1TINUwh[W6mwrDDSGg{ MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB4MUe0O{c,OjZyNkG3OFc9N2F-
A549 MXvGeY5kfGmxbjDBd5NigQ>? M2\6blIwPSEQvF2= NWC3dmQxOjRiaB?= NV\0WJBKTE2VTx?= NXnERmpxcGG|IHGg[4Vv\XKjbDDFUXQhemW4ZYLzZYwh\W[oZXP0xsA> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB4MUe0O{c,OjZyNkG3OFc9N2F-
T24 M4fmfGZ2dmO2aX;uJGF{e2G7 NYDVPZY{Oi93IN88US=> MXSyOEBp M1\UN2ROW09? M36wPIhieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg NUHCfmlPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOlE4PDdpPkK2NFYyPzR5PD;hQi=>
Mia-Paca2 MoXpSpVv[3Srb36gRZN{[Xl? MVWyM|Uh|ryP MXWyOEBp MojvSG1UVw>? NIq1PXRp[XNiYTDn[Y5memGuIFXNWEBz\X[ncoPhcEBm\m[nY4VCpC=> MmjuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNkG3OFcoRjJ4ME[xO|Q4RC:jPh?=
A549 MlPoSpVv[3Srb36gRZN{[Xl? MVSwMlAy6oDVNdMg{txO NFjiOWYzPCCq NYmyXZptTE2VTx?= M3KzbIlv\HWlZYOgV2ZVWEUEoH3SUmEh\XiycnXzd4lwdiCmb4PlJIRmeGWwZHXueIx6 NHj5NVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi0N|AxPSd-MkW4OFMxODV:L3G+
A549 M121fGZ2dmO2aX;uJGF{e2G7 NXTFZW1NOC5yMfMAl|XDqM7:TR?= NIrNOJY4OiCq MV;EUXNQ NV3ocHFH\W6qYX7j[ZMhW1BvRDDwdo91\WmwIHX4dJJme3Orb36gbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZZQh[2:wY3XueJJifGmxboOgc4YhfXBidH:gOeKh|ryPwrC= NWLHUXV{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OFMxODVpPkK1PFQ{ODB3PD;hQi=>
A549 Mo\iSpVv[3Srb36gRZN{[Xl? NGKycXY2yqEQvF2= NIjleFkxNTFiaB?= MmDZSG1UVw>? MmfTbY5kemWjc3XzJGFRNTFiYXP0bZZifGmxbjCgZYZ1\XJiM{CgcYlv MljMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NEOwNFUoRjJ3OESzNFA2RC:jPh?=
Hep3B MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{O1OVAuOjBizszN MkfPOFjDqGh? M1;4eIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M{jBRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW3N|k5Lz5{NE[1O|M6QDxxYU6=
HepG2 NH2ybJhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYnZR4VxOC1{MDFOwG0> M1zydlQ5yqCq MUPk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NE\MN4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
PLC5 NVnt[pFuS2WubDDWbYFjcWyrdImgRZN{[Xl? MnvqNE0zOCEQvF2= MnHvOFjDqGh? MUfk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MljlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N|k5RC:jPh?=
HuH7 NHu5WGNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVGwMVIxKM7:TR?= M{PRR|Q5yqCq M2\JbYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
SK-Hep1 NHvURmxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Moj5NE0zOCEQvF2= NWL2eWpmPDkEoHi= Mn3G[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NGDvVmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
Hep3B M1jmeGFxd3C2b4Ppd{BCe3OjeR?= MYiwMVIxKM7:TR?= NHrqUZk1QMLiaB?= NHrRc5VqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHTvd4Uh\GWyZX7k[Y51dHl? NYDKNmJqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HepG2 NHy5ZphCeG:ydH;zbZMhSXO|YYm= MV[wMVIxKM7:TR?= M1HKOFQ5yqCq NEDNRoFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHTvd4Uh\GWyZX7k[Y51dHl? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
PLC5 NFPtN2VCeG:ydH;zbZMhSXO|YYm= Mk\mNE0zOCEQvF2= MXO0POKhcA>? MmG2bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 M4HSSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW3N|k5Lz5{NE[1O|M6QDxxYU6=
HuH7 MYHBdI9xfG:|aYOgRZN{[Xl? MWCwMVIxKM7:TR?= NEm3UHk1QMLiaB?= M3v0XYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? NULHfYV1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
SK-Hep1 MnT6RZBweHSxc3nzJGF{e2G7 M{TXWFAuOjBizszN MoDsOFjDqGh? M1\UU4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
H1703 MkDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nHUmlEPTB;MD6wOUDPxE1? MlTGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFMoRjJ|N{K5OFA{RC:jPh?=
Sf9 MnXhSpVv[3Srb36gZZN{[Xl? M2nkO|IxKG2rboO= NEC2b29KdmirYnn0bY9vKG:oIH3veZNmKEeVVD3meZNm\CCYRVfGVlIh\XiycnXzd4VlKGmwIGPmPUBqdnOnY4SgZ4VtdHNiYX\0[ZIhOjBibXnud{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyIE2gNE4xOTNizszNMi=> NWrpUGxbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1OVk2OjRpPkG4OVU6PTJ2PD;hQi=>
Sf9 NWeydXZMTnWwY4Tpc44h[XO|YYm= NFz3dnUzOCCvaX7z NFnqT|dKdmirYnn0bY9vKG:oIHj1cYFvKEeVVD3meZNm\CCYRVfGVlIh\XiycnXzd4VlKGmwIGPmPUBqdnOnY4SgZ4VtdHNiYX\0[ZIhOjBibXnud{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyIE2gNE4xOjFizszNMi=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDV3OUWyOEc,OTh3NUm1NlQ9N2F-
NIH3T3 NFXLbo9HfW6ldHnvckBie3OjeR?= MnfsOVAhdk1? MlHZNUBpeg>? MmDDTY5pcWKrdHnvckBw\iCYRVfGVlIhfHKjboPm[YN1\WRiaX6gcY92e2ViTlnIN3Q{KGOnbHzzJIF1KDVyIH7NJIlv[3WkYYTl[EBnd3JiMTDodkBu\WG|dYLl[EBi\nSncjCzNkBpenNid3HzbI92fCCob3zsc5dm\CCkeTDWSWdHKHO2aX31cIF1cW:wIH\vdkAyOCCvaX7zJIJ6KFenc4Tldo4h[myxdITpcoc> NWDOcIJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1OVk2OjRpPkG4OVU6PTJ2PD;hQi=>
HT-29 MUjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Ml3aO|IhcHK| MkTxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iND65JO69VS5? NXr4V|dyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixPVA3PTJpPkK4NVkxPjV{PD;hQi=>
SKOV3 MoH4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NI\BR5Y4OiCqcoO= Mln0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMkiuO|Yh|ryPLh?= M2rGN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUmwOlUzLz5{OEG5NFY2OjxxYU6=
BL21 (DE3) M1L5SmZ2dmO2aX;uJIF{e2G7 NXzNZWtCOzBibXnudy=> MonzTY5pcWKrdHnvckBw\iCKaYO2MZRi\2enZDDNSWxMKGOjdHHsfZRq[yCmb33hbY4hMDFidH:gN|QxKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDFd4Np\XKrY3jpZUBkd2yrIFLMNlEhMESHMzmgZ4VtdHNidYPpcochSmOuLVfMJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkA{OCCvaX7zJIlvKHC{ZYPlcoNmKG:oIGvnZY1u[TN{UG3BWHAh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegcYV1cG:mLDDLbUA:KDBwMEC1OkDPxE1w NIT4XoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO1NVYxPyd-MkizOVE3ODd:L3G+
BL21 (DE3) M4jsUmZ2dmO2aX;uJIF{e2G7 NHH3XHY{OCCvaX7z MXLJcohq[mm2aX;uJI9nKEirc{[teIFo\2WmIF3FUGsh[2G2YXz5eIlkKGSxbXHpckApOSC2bzCzOFAhemW|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFXzZ4hmemmlaHnhJINwdGliQlyyNUApTEV|KTDj[YxteyC3c3nu[{BD[2xvR1ygZZMhe3Wkc4TyZZRmKG2nYYP1doVlKGGodHXyJFMxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiW3fhcY1iOzKSXVHUVEBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFnDOVAhRSByLkC0N{DPxE1w MlK0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|NUG2NFcoRjJ6M{WxOlA4RC:jPh?=
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MCF7 NELUc25CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnTGO|IhcHK| NHW2WZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEiuNlgh|ryPLh?= MnTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6Mk[wPFQoRjJ6OEK2NFg1RC:jPh?=
A549 NYO3eHFtSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MWq3NkBpenN? NEn1dnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEKyMlYzKM7:TT6= NHXUSnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEiyOlA5PCd-Mki4NlYxQDR:L3G+
NIH/3T3 NXH3e2RPTnWwY4Tpc44h[XO|YYm= M3mxbFQzKGi{cx?= NU\rT49MUW6qaXLpeIlwdiCxZjDQSGdHWiCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDy[YNwdWKrbnHueEBpfW2jbjDQSGdHNUKELXnu[JVk\WRiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDR{IHjyd{BjgSClZXzsJJRqfGW{IEm2JIFyfWWxdYOgc45mKHOxbIX0bY9vKGKjc3XkJIF{e2G7LDDJR|UxKD1iMD6wPFUh|ryPLh?= NY\VdlBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOVIxPDVpPkK5NVUzODR3PD;hQi=>
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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
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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[3]
- 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.
    (参考用のみ)
動物試験:[1]
- 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.
    (参考用のみ)

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
混合させたのち直ちに使用することを推奨します。
0.25mg/mL

* 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。

化学情報

分子量 539.62
化学式

C31H33N5O4

CAS No. 656247-17-5
Storage powder
in solvent
別名 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

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04525547 Not yet recruiting Drug: Nintedanib Idiopathic Pulmonary Fibrosis Boehringer Ingelheim December 31 2020 --
NCT04541680 Recruiting Drug: Nintedanib 150 MG [Ofev]|Other: Placebo SARS-Cov-2 Induced Pulmonary Fibrosis Assistance Publique - Hôpitaux de Paris|Boehringer Ingelheim October 29 2020 Phase 3
NCT03283007 Recruiting Drug: Nintedanib|Drug: Placebo Lung-transplant Recipients Assistance Publique - Hôpitaux de Paris October 30 2019 Phase 3
NCT03958071 Completed Drug: Nintedanib|Drug: Pirfenidone|Other: Untreated Cohort Idiopathic Pulmonary Fibrosis Boehringer Ingelheim February 1 2019 --
NCT03710824 Recruiting Drug: Nintedanib Idiopathic Pulmonary Fibrosis Boehringer Ingelheim February 28 2019 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

相関VEGFR製品

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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