Nintedanib (BIBF 1120)

For research use only. Not for use in humans.

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

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
5mg	JPY 21900
50mg	JPY 113200
200mg	JPY 212800

最寄りの販売代理店を探す

東京
北海道
東北
北関東
南関東
東海
北信越
近畿
中国
四国
九州

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

代表番号: 03-5615-9297 | 電子メール：[email protected]

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

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)	もっとクリックする
13 nM	13 nM	16 nM	26 nM	34 nM	もっとクリックする

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?=
HT-29	NEXaO2hCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NX7oVo82PzJiaILz		NHXwdIVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCwMlg{KM7:TT6=	Mlf5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6Mk[wPFQoRjJ6OEK2NFg1RC:jPh?=
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=>
Sf9	NUS0e4RzTnWwY4Tpc44h[XO\|YYm=				MlfmTY5pcWKrdHnvckBw\iCqdX3hckBXTUeIUkKg[ZhxemW\|c3XkJIlvKFOoOTDj[YxteyxiSVO1NEA:KDBwMEC1JO69VS5?	NUDPc5FnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1NlI1PjVpPkG5OVIzPDZ3PD;hQi=>
NIH3T3	NX;BW2pjTnWwY4Tpc44h[XO\|YYm=		NX:5NGNlOSCqch?=		NF7zU\|dKdmirYnn0bY9vKG:oIG\FS2Yue3SrbYXsZZRm\CCqdX3hckBXTUeIUkKgdIhwe3Cqb4L5cIF1cW:wIHX4dJJme3OnZDDpckBud3W\|ZTDOTWg{XDNiY3XscJMheHKndILlZZRm\CCob4KgNUBpeiCvZXHzeZJm\CB\|MjDodpMh[W[2ZYKg[JJ2\yCmb4PlJIJ6KGmvbYXuc5Bz\WOrcHn0ZZRqd25iYnHz[YQheHWuc3WtZ4hie2ViZYjw[ZJqdWWwdB?=	NFHBZ4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUWyNlQ3PSd-MUm1NlI1PjV:L3G+
BRP	M3zwNGFxd3C2b4Ppd{Bie3OjeR?=				MnLZTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDCVnAh[2WubIOgZZN{\XO\|ZXSgZZMh[2G\|cHHz[U0{KGOuZXH2ZYdm	MnezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3MkK0OlUoRjF7NUKyOFY2RC:jPh?=
BRP	MkD3RY51cWGwZ3nv[4VvcWNiYYPzZZk>				NH;BNG9CdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDCVnAh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZpkhYzOKXYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGG\|c3H5	MnvuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3MkK0OlUoRjF7NUKyOFY2RC:jPh?=
TC32	M33VcJFJXFNiYYPzZZk>				NFTnPWhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?=	M33YR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673	M{jMWZFJXFNiYYPzZZk>				NXvHeop4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFG2O\|Mh[2WubIO=	M4LPUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY	MV3xTHRUKGG\|c3H5				NETqTGxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?=	NEH5WWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	NIHnXZhyUFSVIHHzd4F6				M3j3Z5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	NF22RoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-37	NV:zSXhHeUiWUzDhd5NigQ>?				NVTOR3FNeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-SH	NE\od2lyUFSVIHHzd4F6				MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?=	M1TqSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643	M{j3UpFJXFNiYYPzZZk>				M3W2O5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	NGLjfJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	NW\sN4tweUiWUzDhd5NigQ>?				NILXUZlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz	MoL4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	MUfxTHRUKGG\|c3H5				NGD0ZYNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBNSU5vNTDj[Yxtew>?	MoPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
DAOY	M3ridJFJXFNiYYPzZZk>				Mk\mdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgSGFQYSClZXzsdy=>	MkHvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	MVHxTHRUKGG\|c3H5				MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>?	MkTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R)	M3fNSpFJXFNiYYPzZZk>				NYDxTWpseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh30	MVnxTHRUKGG\|c3H5				NGraSWdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDNyIHPlcIx{	NIrMTGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
U-2 OS	MkDCdWhVWyCjc4PhfS=>				NULEOJNEeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy\|	NIT2XpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	MWHxTHRUKGG\|c3H5				MnnkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgU2hUNTVyIHPlcIx{	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh41	M{j5XJFJXFNiYYPzZZk>				NHPaRVhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{	M1TnfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2	NVXYVGRKeUiWUzDhd5NigQ>?				MnjPdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	MoPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	MlTjdWhVWyCjc4PhfS=>				NIf1VYtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=>	NVnY[Zc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5	NGjkRnVyUFSVIHHzd4F6				NE\UZmZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO=	M3zQNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643	MmCzdWhVWyCjc4PhfS=>				MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORlE3PDNiY3XscJM>	M3\qN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	NUXze3RneUiWUzDhd5NigQ>?				M1LGeJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN?	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
TC32	MVvxTHRUKGG\|c3H5				NF2zO4tyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{	NV\ne5B6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18	NUi0WZhieUiWUzDhd5NigQ>?				Mn\XdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVogyQCClZXzsdy=>	NH\McIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+

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アッセイ

Methods	Test Index	PMID
Western blot	Fibronectin / Collagen 1a1; PubMed: 26072676 Am J Respir Cell Mol Biol (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 Am J Respir Cell Mol Biol 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 Sci Rep 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 Cancer Sci 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 Sci Rep 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)

参考

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 Nintedanib (BIBF 1120) SDFをダウンロードする

分子量	539.62
化学式	C₃₁H₃₃N₅O₄
CAS No.	656247-17-5
Storage	3 years-20°C powder 2 years-80°C 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

投与体積（動物毎）

動物数

匹

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

計算結果:

投与溶媒濃度： mg/ml；

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL，注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。）

投与溶媒調製方法：μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

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

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
初めの濃度：
稀釈倍数：

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：

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 (data from https://clinicaltrials.gov, updated on 2021-01-06)

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
*大学・企業名:
*名前:
*電子メール:
*電話番号:
*内容:

VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

Selective VEGFR Inhibitors

Vandetanib (ZD6474) : VEGFR2-selective, IC50=40 nM.
Most Potent VEGFR Inhibitor

Cabozantinib (XL184, BMS-907351) : VEGFR2, IC50=0.035 nM.
FDA-approved VEGFR Inhibitor

Axitinib : Approved by FDA for Renal Cell Carcinoma.
Classic VEGFR Inhibitor

Dovitinib (TKI-258, CHIR-258) : Multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM.

相関VEGFR製品

SU5402

SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Erlotinib

Erlotinib (CP358774, NSC 718781, OSI-774) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Bemcentinib (R428)

Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.
Axitinib

Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

Features:Superior as second-line therapy relative to sorafenib (current standard-of-care).
Cabozantinib (BMS-907351)

Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
Vandetanib (ZD6474)

Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).

研究分野別

製品類型

Nintedanib (BIBF 1120)

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

お薦めの試験操作（参考用のみ）

参考

溶解度 (25°C)

化学情報 Nintedanib (BIBF 1120) SDFをダウンロードする

投与溶媒組成計算器(クリア溶液)

便利ツール

モル濃度計算器

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

希釈計算器

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

連続希釈計算器方程式

連続希釈剤

計算結果

分子量计算器

総分子量：g/mol

モル濃度計算器

臨床試験 (data from https://clinicaltrials.gov, updated on 2021-01-06)

技術サポート

VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

相関VEGFR製品