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Nintedanib (BIBF 1120)

目录号：S1010 别名: Intedanib, Vargatef, Ofev 中文名称：尼达尼布

仅限科研使用

Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 尼达尼布是一种有效的三重血管激酶抑制剂，作用于VEGFR1/2/3， FGFR1/2/3和PDGFRα/β，在无细胞试验中IC50分别为34 nM/13 nM/13 nM， 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。

Nintedanib (BIBF 1120) Chemical Structure

CAS: 656247-17-5

规格	价格	库存
10mM (1mL in DMSO)	RMB 1970.51	现货
5mg	RMB 991.25	现货
50mg	RMB 5492.96	现货
200mg	RMB 10401.3	现货
大包装	有超大折扣

今日订购，明日送达全国免运费分装免费分装成小规格产品（单支最小为1mg）如1支10mg产品可分装为10支1mg产品全国免费电话：400-668-6834 \| Email：info@selleck.cn

客户使用Selleck生产的Nintedanib (BIBF 1120)发表文献109篇：

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述

靶点

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)	点击更多
13 nM	13 nM	16 nM	26 nM	34 nM	点击更多

体外研究

BIBF1120对酪氨酸激酶受体如EGFR, HER2, InsR, IGF1R 或者细胞周期激酶 CDK1, CDK2 和CDK4抑制效果不大， IC50都大于1x10³nM。BIBF1120强抑制VEGF-刺激的HUVEC 和VEGF-刺激的HSMEC，EC50分别为9 和 7 nM。相反，BIBF1120 作用于FaDu, Calu-6 和Hela时EC50则大到几百倍。^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

SKOV3	MoDGSpVv[3Srb36gRZN{[Xl?	Mn:5OUDDvU1?	M{Hp[lI1KGh?	NV;RVYsyTE2VTx?=	Mo\nbY5lfWOnczDhJJNq\26rZnnjZY51KGmwY4LlZZNmKGmwIITo[UBxem:vb4TldkBi[3Srdnn0bYV{KG:oIFWtZ4FlNMLiQ1TINUwh[W6mwrDDSGg{	M1HobFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4ME[xO\|Q4Lz5{NkC2NVc1PzxxYU6=
A549	Ml7sSpVv[3Srb36gRZN{[Xl?	MWqyM\|Uh\|ryP	MoHRNlQhcA>?	M4f6UGROW09?	MmLibIF{KGFiZ3Xu[ZJidCCHTWSgdoV3\XK\|YXyg[YZn\WO2wrC=	M2q0SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4ME[xO\|Q4Lz5{NkC2NVc1PzxxYU6=
T24	Ml\PSpVv[3Srb36gRZN{[Xl?	NVLVZpR[Oi93IN88US=>	MlHuNlQhcA>?	NUPud3hjTE2VTx?=	MXjoZZMh[SCpZX7ldoFtKEWPVDDy[ZZmenOjbDDl[oZm[3UEoB?=	NVO5WGo6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOlE4PDdpPkK2NFYyPzR5PD;hQi=>
Mia-Paca2	NIS1d2xHfW6ldHnvckBCe3OjeR?=	MVmyM\|Uh\|ryP	NVjWfFVSOjRiaB?=	NX\YZnZJTE2VTx?=	Mnr4bIF{KGFiZ3Xu[ZJidCCHTWSgdoV3\XK\|YXyg[YZn\WO2wrC=	NEnvXYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC2NVc1Pyd-Mk[wOlE4PDd:L3G+
A549	M4nWfWZ2dmO2aX;uJGF{e2G7	Ml;wNE4xOeLCk{ZCpO69VQ>?	NEfVbJkzPCCq	NUPIUWFMTE2VTx?=	NHLiXFRqdmS3Y3XzJHNHXFCGwrDtVm5CKGW6cILld5Nqd25iZH;z[UBl\XCnbnTlcpRtgQ>?	NELIWXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi0N\|AxPSd-MkW4OFMxODV:L3G+
A549	NXvJc4NzTnWwY4Tpc44hSXO\|YYm=	M1\MPFAvODIkgKO1xsDPxE1?	NWG0dlB1PzJiaB?=	NGfrZoJFVVOR	M3jrUYVvcGGwY3XzJHNRNURicILveIVqdiCneIDy[ZN{cW:wIHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{IHH0JINwdmOnboTyZZRqd26\|IH;mJJVxKHSxIEZCpO69VcLi	NF;UeWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi0N\|AxPSd-MkW4OFMxODV:L3G+
A549	Mm\PSpVv[3Srb36gRZN{[Xl?	NEXKW2s2yqEQvF2=	MX[wMVEhcA>?	NVfIRWRnTE2VTx?=	MYnpcoNz\WG\|ZYOgRXAuOSCjY4TpeoF1cW:wIDDh[pRmeiB\|MDDtbY4>	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh2M{CwOUc,OjV6NEOwNFU9N2F-
Hep3B	Mlu5R4VtdCCYaXHibYxqfHliQYPzZZk>	NFfqZWExNTJyIN88US=>	M4PmVVQ5yqCq		MV3k[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	M3XBU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW3N\|k5Lz5{NE[1O\|M6QDxxYU6=
HepG2	NXXGcIZVS2WubDDWbYFjcWyrdImgRZN{[Xl?	NUmwV\|F2OC1{MDFOwG0>	MW[0POKhcA>?		M3zWS4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	MoXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N\|k5RC:jPh?=
PLC5	M4G4NGNmdGxiVnnhZoltcXS7IFHzd4F6	NV76b5hDOC1{MDFOwG0>	NFO4Xpo1QMLiaB?=		M1L6TYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
HuH7	MmD3R4VtdCCYaXHibYxqfHliQYPzZZk>	NGTsfGkxNTJyIN88US=>	MU[0POKhcA>?		M332[YRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	MkTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N\|k5RC:jPh?=
SK-Hep1	NFK2OVBE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	M2H5TVAuOjBizszN	MWK0POKhcA>?		MVLk[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	MkO5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N\|k5RC:jPh?=
Hep3B	NXW4cVM2SXCxcITvd4l{KEG\|c3H5	MWWwMVIxKM7:TR?=	MkfiOFjDqGh?		NYOwdm1QcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
HepG2	MkLERZBweHSxc3nzJGF{e2G7	MUiwMVIxKM7:TR?=	Mlr6OFjDqGh?		NWDpVYplcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7	MofvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N\|k5RC:jPh?=
PLC5	MoOyRZBweHSxc3nzJGF{e2G7	M{S3eVAuOjBizszN	M2nKU\|Q5yqCq		NFrmfZVqdmS3Y3XzJINmdGxiYYDvdJRwe2m\|IHTvd4Uh\GWyZX7k[Y51dHl?	M2jxSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW3N\|k5Lz5{NE[1O\|M6QDxxYU6=
HuH7	M1m4bWFxd3C2b4Ppd{BCe3OjeR?=	NXz3eoh2OC1{MDFOwG0>	M1nST\|Q5yqCq		M3vR[olv\HWlZYOgZ4VtdCCjcH;weI9{cXNiZH;z[UBl\XCnbnTlcpRtgQ>?	NXvSe4dXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
SK-Hep1	MkG1RZBweHSxc3nzJGF{e2G7	M4XtNlAuOjBizszN	NIKzNpc1QMLiaB?=		NIDlfHZqdmS3Y3XzJINmdGxiYYDvdJRwe2m\|IHTvd4Uh\GWyZX7k[Y51dHl?	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
H1703	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NWfmSnViUUN3ME2wMlA2KM7:TR?=	NVPI[Wo1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODNpPkKzO\|I6PDB\|PD;hQi=>
Sf9	NFvCdWFHfW6ldHnvckBie3OjeR?=		MUiyNEBucW6\|		NYP6cop6UW6qaXLpeIlwdiCxZjDtc5V{\SCJU2St[pV{\WRiVlXHSnIzKGW6cILld5Nm\CCrbjDT[lkhcW6\|ZXP0JINmdGy\|IHHmeIVzKDJyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvODF\|IN88UU4>	NXrwNW4xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1OVk2OjRpPkG4OVU6PTJ2PD;hQi=>
Sf9	M3e4TWZ2dmO2aX;uJIF{e2G7		NH31cVMzOCCvaX7z		M2fUb2lvcGmkaYTpc44hd2ZiaIXtZY4hT1OWLX\1d4VlKF[HR1\SNkBmgHC{ZYPz[YQhcW5iU3[5JIlve2WldDDj[YxteyCjZoTldkAzOCCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTBiPTCwMlAzOSEQvF2u	MnzjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh3NUm1NlQoRjF6NUW5OVI1RC:jPh?=
NIH3T3	M3vV[GZ2dmO2aX;uJIF{e2G7	M4HiN\|UxKG6P	M2HmWVEhcHJ?		MXTJcohq[mm2aX;uJI9nKF[HR1\SNkB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCQSVizWFMh[2WubIOgZZQhPTBibl2gbY5kfWKjdHXkJIZweiBzIHjyJI1m[XO3cnXkJIFnfGW{IEOyJIhzeyC5YYPoc5V1KG[xbHzve4VlKGK7IG\FS2Yhe3SrbYXsZZRqd25iZn;yJFExKG2rboOgZpkhX2W\|dHXyckBjdG:2dHnu[y=>	M2fuflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NUW5OVI1Lz5zOEW1PVUzPDxxYU6=
HT-29	MWrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NHrQTJg4OiCqcoO=		NIrFNXdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTC0Mlkh\|ryPLh?=	MnnHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzOUC2OVIoRjJ6MUmwOlUzRC:jPh?=
SKOV3	M4[4eWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		M4XXNFczKGi{cx?=		NUG0W2tQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyIE2gNlgvPzZizszNMi=>	NHfQUZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG5NFY2Oid-MkixPVA3PTJ:L3G+
BL21 (DE3)	M3\Sb2Z2dmO2aX;uJIF{e2G7		NEP2bXc{OCCvaX7z		NGDMTWtKdmirYnn0bY9vKG:oIFjpd\|YufGGpZ3XkJG1GVEtiY3H0ZYx6fGmlIHTvcYFqdiBqMTD0c{A{PDBicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGV{[2incnnjbIliKGOxbHmgRmwzOSBqRFWzLUBk\WyuczD1d4lv\yCEY3ytS2wh[XNic4Xid5Rz[XSnIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMhcW5icILld4Vv[2Vib3[gX4didW2jM{LQYWFVWCCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[{Bu\XSqb3SsJGtqKD1iMD6wNFU3KM7:TT6=	NIHYdWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO1NVYxPyd-MkizOVE3ODd:L3G+
BL21 (DE3)	M2rkdGZ2dmO2aX;uJIF{e2G7		MYqzNEBucW6\|		MnrBTY5pcWKrdHnvckBw\iCKaYO2MZRi\2enZDDNSWxMKGOjdHHsfZRq[yCmb33hbY4hMDFidH:gN\|QxKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDFd4Np\XKrY3jpZUBkd2yrIFLMNlEhMESHMzmgZ4VtdHNidYPpcochSmOuLVfMJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkA{OCCvaX7zJIlvKHC{ZYPlcoNmKG:oIGvnZY1u[TN{UG3BWHAh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegcYV1cG:mLDDJR\|UxKD1iMD6wOFMh\|ryPLh?=	M17GW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{WxOlA4Lz5{OEO1NVYxPzxxYU6=
HT-29	NWjxb5FRSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MlG1O\|IhcHK\|		Mmi3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxKD1iMD64N{DPxE1w	MkPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6Mk[wPFQoRjJ6OEK2NFg1RC:jPh?=
MCF7	MlvSRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MUO3NkBpenN?		MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDhwMkig{txONg>?	Mk\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6Mk[wPFQoRjJ6OEK2NFg1RC:jPh?=
A549	M2XNTmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MmrGO\|IhcHK\|		NFWyepJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEKyMlYzKM7:TT6=	NYf1OlRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4NlYxQDRpPkK4PFI3ODh2PD;hQi=>
NIH/3T3	M1rpdGZ2dmO2aX;uJIF{e2G7		M{ToV\|QzKGi{cx?=		M3exUWlvcGmkaYTpc44hd2ZiUFTHSnIhcW5ibX;1d4UhVkmKL{PUN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icnXjc41jcW6jboSgbJVu[W5iUFTHSk1DSi2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA1OiCqcoOgZpkh[2WubDD0bZRmeiB7NjDhdZVmd3W\|IH;u[UB{d2y3dHnvckBj[XOnZDDhd5NigSxiSVO1NEA:KDBwMEi1JO69VS5?	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF3MkC0OUc,OjlzNUKwOFU9N2F-
Sf9	NELjPGlHfW6ldHnvckBie3OjeR?=				NIO0RYhKdmirYnn0bY9vKG:oIHj1cYFvKF[HR1\SNkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy\|LDDJR\|UxKD1iMD6wNFUh\|ryPLh?=	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV{MkS2OUc,OTl3MkK0OlU9N2F-
NIH3T3	M1zzUWZ2dmO2aX;uJIF{e2G7		MVGxJIhz		NWj3Sph5UW6qaXLpeIlwdiCxZjDWSWdHNXO2aX31cIF1\WRiaIXtZY4hXkWJRmKyJJBpd3OyaH;yfYxifGmxbjDlfJBz\XO\|ZXSgbY4hdW:3c3WgUmlJO1R\|IHPlcIx{KHC{ZYTy[YF1\WRiZn;yJFEhcHJibXXhd5Vz\WRiM{KgbJJ{KGGodHXyJIRzfWdiZH;z[UBjgSCrbX31co9xemWlaYDpeIF1cW:wIHLhd4VlKHC3bIPlMYNp[XOnIHX4dIVzcW2nboS=	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV{MkS2OUc,OTl3MkK0OlU9N2F-
BRP	MnrJRZBweHSxc3nzJIF{e2G7				Mm\jTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDCVnAh[2WubIOgZZN{\XO\|ZXSgZZMh[2G\|cHHz[U0{KGOuZXH2ZYdm	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV{MkS2OUc,OTl3MkK0OlU9N2F-
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SK-N-MC	NGDvd2pyUFSVIHHzd4F6				NVTMWZNoeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	M4LhRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32	M4j1R5FJXFNiYYPzZZk>				M2\RXpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM>	NVPlTlFHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18	Ml[0dWhVWyCjc4PhfS=>				NHX3T4tyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDF6IHPlcIx{	Ml7mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=

Click to View More Cell Line Experimental Data

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

体内研究

在小鼠的Fadu 移植瘤中，按鼠体重，每千克处理100mg BIBF1120,结果显示肿瘤血管密度降低76%。BIBF1120 作用于移植瘤模型Caki-1, HT-29, SKOV-3, Calu6 和PAC-120同样有显著的抑制效果。BIBF1120已用于治疗多种癌症，包括：非小细胞肺癌，前列腺癌，卵巢癌，及结肠直肠癌。且BIBF1120目前处于二期临床实验阶段。^[1]

激酶实验：^[1]	激酶实验: VEGFR-2的胞质酪氨酸激酶域克隆到pFastBac载体上，与谷胱甘肽巯基转移酶 (GST)相融合。 GST融合蛋白在SF-9昆虫细胞中表达，用重元素萃取分离法提取。HEPEX萃取液包括20 mM HEPES （pH 为7.4）, 100 mM NaCl, 10 mM ss-甘油磷酸盐, 10 mM 聚硝基磷酸单苯酯, 30mM NaF, 5 mM EDTA, 5% 甘油, 1% Triton X-100, 1 mM Na₃VO₄, 0.1% SDS, 0.5μg/ml 抑肽素A, 2.5 μg/ml 3,4-二氯异香豆素(丝氨酸蛋白酶的不可逆抑制剂), 2.5 μg/ml反式-环氧琥珀酰-L-亮氨酰-L-氨基丁烷, 20 KIU/ml 抑肽酶, 2 μg/ml 亮抑肽酶, 1 mM苯甲脒，和0.002% PMSF。谷氨酸和酪氨酸按4:1比例随机组成的聚合物作为基底物，每组50ul的反应液包括5 % DMSO, 40 mM HEPES （pH 为 7.4）, 5 mM MgCl₂, 5 mM MnCl₂, 0.5 mg/ml 聚谷氨酸/酪氨酸, 0.05% Triton X-100, 100 μM ATP, 1 μCi [γ-³³P]ATP ，和 10 μl酶制剂。实验在室温下进行20分钟，最后加入10 μl 5 % H₃PO₄终止反应。沉淀物转移到GF/B 过滤器中，使用与96孔过滤器相配的万能采集器收集。通过闪烁计数器测定混合物的放射能。
细胞实验：^[1]	Cell lines: HUVEC, HUASMC,和BRP细胞系 Concentrations: 50 nM Incubation Time: 2小时 Method: 不同的肿瘤细胞系在96孔板上培养24小时。然后加入不同浓度的BIBF1120，处理72小时。通过Alamar-Blue染色的荧光强度测试EC50值。
动物实验：^[1]	Animal Models: 雌性无胸腺NMRI-nu/nu鼠 Dosages: 100 mg/kg Administration: 口服处理

参考文献	[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 [3] Roth GJ, et al. J Med Chem, 2009, 52(14), 4466-4480.

溶解度（25°C）

体外


体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 5% DMSO+40% PEG 300+2% Tween 80+ddH2O 点击购买： PEG300 Tween 80	0.25mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量	539.62
化学式	C₃₁H₃₃N₅O₄
CAS号	656247-17-5
储存条件	3年	-20°C	粉状
储存条件	2年	-80°C	溶于溶剂

Download Nintedanib (BIBF 1120) SDF

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

临床试验信息

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)

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