Nintedanib (BIBF 1120)

For research use only. Not for use in humans.

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

Nintedanib (BIBF 1120) Chemical Structure

CAS No. 656247-17-5

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1970.51 现货
RMB 991.25 现货
RMB 1719.62 现货
RMB 5492.96 现货
RMB 10401.3 现货
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客户使用Selleck生产的Nintedanib (BIBF 1120)发表文献86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 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。
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)
13 nM 13 nM 16 nM 26 nM 34 nM
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 M{HxcGZ2dmO2aX;uJGF{e2G7 MoiyOUDDvU1? NHWyOWUzPCCq M3HCUWROW09? MXXpcoR2[2W|IHGgd4lodmmoaXPhcpQhcW6lcnXhd4UhcW5idHjlJJBzd22xdHXyJIFkfGm4aYTp[ZMhd2ZiRT3jZYQtyqCFRFixMEBidmUEoFPETFM> NGi5NZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC2NVc1Pyd-Mk[wOlE4PDd:L3G+
A549 MVnGeY5kfGmxbjDBd5NigQ>? M{DzUlIwPSEQvF2= M2jWXVI1KGh? MXrEUXNQ M2XWbohieyCjIHflcoVz[WxiRV3UJJJmfmW{c3HsJIVn\mWldNMg NFP1XVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC2NVc1Pyd-Mk[wOlE4PDd:L3G+
T24 NG\ZNWNHfW6ldHnvckBCe3OjeR?= MUmyM|Uh|ryP NWH2NJB1OjRiaB?= M13IT2ROW09? NVvRUHg2cGG|IHGg[4Vv\XKjbDDFUXQhemW4ZYLzZYwh\W[oZXP0xsA> Ml7EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNkG3OFcoRjJ4ME[xO|Q4RC:jPh?=
Mia-Paca2 NYHkTmx2TnWwY4Tpc44hSXO|YYm= NGPQSHczNzVizszN MmCwNlQhcA>? M1fGXGROW09? Mn;4bIF{KGFiZ3Xu[ZJidCCHTWSgdoV3\XK|YXyg[YZn\WO2wrC= NWHwdWZLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOlE4PDdpPkK2NFYyPzR5PD;hQi=>
A549 NWPlc|F2TnWwY4Tpc44hSXO|YYm= NX\wNJR[OC5yMfMAl|XDqM7:TR?= NHS0NnUzPCCq NUOyd4ZVTE2VTx?= NV7mVoVYcW6mdXPld{BUTlSSRNMgcXJPSSCneIDy[ZN{cW:wIHTvd4Uh\GWyZX7k[Y51dHl? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh2M{CwOUc,OjV6NEOwNFU9N2F-
A549 NFq2d3dHfW6ldHnvckBCe3OjeR?= MlXCNE4xOeLCk{ZCpO69VQ>? NXLXd3RSPzJiaB?= NV25cFFKTE2VTx?= MXvlcohidmOnczDTVE1FKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meiCjdDDjc45k\W62cnH0bY9veyCxZjD1dEB1dyB3wrFOwG3DqA>? NI\5XoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi0N|AxPSd-MkW4OFMxODV:L3G+
A549 MnTFSpVv[3Srb36gRZN{[Xl? MVS1xsDPxE1? NG\ZeYQxNTFiaB?= MmjOSG1UVw>? MojEbY5kemWjc3XzJGFRNTFiYXP0bZZifGmxbjCgZYZ1\XJiM{CgcYlv MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh2M{CwOUc,OjV6NEOwNFU9N2F-
Hep3B NUW3O|VqS2WubDDWbYFjcWyrdImgRZN{[Xl? M1jMV|AuOjBizszN MVu0POKhcA>? M1L3boRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MojaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N|k5RC:jPh?=
HepG2 MlntR4VtdCCYaXHibYxqfHliQYPzZZk> NFXsWJoxNTJyIN88US=> NWnBVGJkPDkEoHi= MUnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M3;TOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW3N|k5Lz5{NE[1O|M6QDxxYU6=
PLC5 NFr1eWRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXLEcHRDOC1{MDFOwG0> M4fZUlQ5yqCq MWXk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NWfWOXNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HuH7 MnPNR4VtdCCYaXHibYxqfHliQYPzZZk> MYqwMVIxKM7:TR?= M{H5c|Q5yqCq M2Xw[YRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MkG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N|k5RC:jPh?=
SK-Hep1 MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVPvbllSOC1{MDFOwG0> MXq0POKhcA>? MVrk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MmfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUezPVgoRjJ2NkW3N|k5RC:jPh?=
Hep3B MonzRZBweHSxc3nzJGF{e2G7 NF;3PGwxNTJyIN88US=> MV[0POKhcA>? Mlj6bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NWPFVY5ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVc{QThpPkK0OlU4Ozl6PD;hQi=>
HepG2 MoK5RZBweHSxc3nzJGF{e2G7 Mo\0NE0zOCEQvF2= MWK0POKhcA>? MUHpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> NF7EV|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
PLC5 MWDBdI9xfG:|aYOgRZN{[Xl? Mnf4NE0zOCEQvF2= MXm0POKhcA>? NF7PXY1qdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHTvd4Uh\GWyZX7k[Y51dHl? NFjKWHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
HuH7 NIWyfmRCeG:ydH;zbZMhSXO|YYm= NVrFT21wOC1{MDFOwG0> NXHCU2RFPDkEoHi= MWLpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGSxc3Wg[IVx\W6mZX70cJk> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3N{O5PEc,OjR4NUezPVg9N2F-
SK-Hep1 MnzyRZBweHSxc3nzJGF{e2G7 M1\IUFAuOjBizszN MYW0POKhcA>? MmX6bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCmb4PlJIRmeGWwZHXueIx6 NHfxW289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1O|M6QCd-MkS2OVc{QTh:L3G+
H1703 NWjJVYdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvLeWY{UUN3ME2wMlA2KM7:TR?= NVrGN2FURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODNpPkKzO|I6PDB|PD;hQi=>
Sf9 M2qxTWZ2dmO2aX;uJIF{e2G7 MXeyNEBucW6| NGPSWlhKdmirYnn0bY9vKG:oIH3veZNmKEeVVD3meZNm\CCYRVfGVlIh\XiycnXzd4VlKGmwIGPmPUBqdnOnY4SgZ4VtdHNiYX\0[ZIhOjBibXnud{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyIE2gNE4xOTNizszNMi=> NUDpRYU5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1OVk2OjRpPkG4OVU6PTJ2PD;hQi=>
Sf9 NFGzdYRHfW6ldHnvckBie3OjeR?= NXPiVHpTOjBibXnudy=> MVzJcohq[mm2aX;uJI9nKGi3bXHuJGdUXC2odYPl[EBXTUeIUkKg[ZhxemW|c3XkJIlvKFOoOTDpcpNm[3RiY3XscJMh[W[2ZYKgNlAhdWmwczDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDJR|UxKD1iMD6wNlEh|ryPLh?= NFjlWJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEW1PVUzPCd-MUi1OVk2OjR:L3G+
NIH3T3 M2XQZmZ2dmO2aX;uJIF{e2G7 Mke2OVAhdk1? MWCxJIhz MkL2TY5pcWKrdHnvckBw\iCYRVfGVlIhfHKjboPm[YN1\WRiaX6gcY92e2ViTlnIN3Q{KGOnbHzzJIF1KDVyIH7NJIlv[3WkYYTl[EBnd3JiMTDodkBu\WG|dYLl[EBi\nSncjCzNkBpenNid3HzbI92fCCob3zsc5dm\CCkeTDWSWdHKHO2aX31cIF1cW:wIH\vdkAyOCCvaX7zJIJ6KFenc4Tldo4h[myxdITpcoc> NX\CWGhyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1OVk2OjRpPkG4OVU6PTJ2PD;hQi=>
HT-29 M2i5ZmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MmLJO|IhcHK| NHnab|JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC0Mlkh|ryPLh?= M3jselxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUmwOlUzLz5{OEG5NFY2OjxxYU6=
SKOV3 M3vYb2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NETY[GU4OiCqcoO= MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB{OD63OkDPxE1w NWrBdG1FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixPVA3PTJpPkK4NVkxPjV{PD;hQi=>
BL21 (DE3) NVvpUG53TnWwY4Tpc44h[XO|YYm= M3TzelMxKG2rboO= NVLFTGhWUW6qaXLpeIlwdiCxZjDIbZM3NXSjZ3fl[EBOTUyNIHPheIFtgXSrYzDkc41icW5iKEGgeI8hOzRyIILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJGJNOjFiKFTFN{kh[2WubIOgeZNqdmdiQnPsMWdNKGG|IIP1ZpN1emG2ZTDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGmwIIDy[ZNmdmOnIH;mJHto[W2vYUOyVH1CXFBiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcochdWW2aH;kMEBMcSB;IECuNFA2PiEQvF2u M1TNd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{WxOlA4Lz5{OEO1NVYxPzxxYU6=
BL21 (DE3) M3vhTmZ2dmO2aX;uJIF{e2G7 MUOzNEBucW6| MXjJcohq[mm2aX;uJI9nKEirc{[teIFo\2WmIF3FUGsh[2G2YXz5eIlkKGSxbXHpckApOSC2bzCzOFAhemW|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFXzZ4hmemmlaHnhJINwdGliQlyyNUApTEV|KTDj[YxteyC3c3nu[{BD[2xvR1ygZZMhe3Wkc4TyZZRmKG2nYYP1doVlKGGodHXyJFMxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiW3fhcY1iOzKSXVHUVEBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFnDOVAhRSByLkC0N{DPxE1w NIPPZ|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO1NVYxPyd-MkizOVE3ODd:L3G+
HT-29 NIqyd5hCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2rwSlczKGi{cx?= NYLHPWtXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE45OyEQvF2u NWOxN2RzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4NlYxQDRpPkK4PFI3ODh2PD;hQi=>
MCF7 NVr3cI9wSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NXW2cJBIPzJiaILz NVzvWVhWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC4MlI5KM7:TT6= MmXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6Mk[wPFQoRjJ6OEK2NFg1RC:jPh?=
A549 NH3NdXNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEnxO|c4OiCqcoO= NYTYdoxrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCyNk43OiEQvF2u M4LCZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEK2NFg1Lz5{OEiyOlA5PDxxYU6=
NIH/3T3 M4X2XmZ2dmO2aX;uJIF{e2G7 NWnzXZFoPDJiaILz NWjh[4hkUW6qaXLpeIlwdiCxZjDQSGdHWiCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDy[YNwdWKrbnHueEBpfW2jbjDQSGdHNUKELXnu[JVk\WRiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDR{IHjyd{BjgSClZXzsJJRqfGW{IEm2JIFyfWWxdYOgc45mKHOxbIX0bY9vKGKjc3XkJIF{e2G7LDDJR|UxKD1iMD6wPFUh|ryPLh?= Mo\SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzNUKwOFUoRjJ7MUWyNFQ2RC:jPh?=
Sf9 NVvLelV1TnWwY4Tpc44h[XO|YYm= MWHJcohq[mm2aX;uJI9nKGi3bXHuJHZGT0[UMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwJF0hOC5yMEWg{txONg>? NV;uPYVRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1NlI1PjVpPkG5OVIzPDZ3PD;hQi=>
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... 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
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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验：[1]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验：[1]
- 合并
  • Animal Models: 雌性无胸腺NMRI-nu/nu鼠
  • Dosages: 100 mg/kg
  • Administration: 口服处理
    (Only for Reference)

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 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
 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 粉状
溶于溶剂
别名 Intedanib, Vargatef, Ofev

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 ul 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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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 --

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

相关VEGFR产品

  • SU5402 New

    SU5402是一种有效的多靶点受体激酶抑制剂，对VEGFR2，FGFR1，和PDGF-Rβ的IC50分别为20 nM，30 nM，和510 nM。

  • Erlotinib New

    Erlotinib (CP358774, NSC 718781)是一种EGFR抑制剂，IC50 为 2 nM，对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。Erlotinib可诱导自噬。

  • Bemcentinib (R428) New

    Bemcentinib (R428, BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。

  • Regorafenib (BAY 73-4506)

    Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 是一个多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR-β，Kit (c-Kit)，RET (c-RET)和Raf-1，在无细胞试验中IC50分别是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。Regorafenib 可诱导自噬。

    Features:Regorafenib是一个新的口服多激酶抑制剂。

  • Axitinib

    Axitinib (AG 013736)是一种多靶点抑制剂，作用于 VEGFR1，VEGFR2，VEGFR3，PDGFRβ和c-Kit，在猪主动脉内皮细胞中IC50分别为0.1 nM，0.2 nM，0.1-0.3 nM，1.6 nM和1.7 nM。

    Features:Axitinib与目前使用的sorafenib相比，作为二代治疗法，更有效。

  • Cabozantinib (BMS-907351)

    Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分别为1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。

  • Vandetanib (ZD6474)

    Vandetanib (ZD6474) 是一种有效的 VEGFR2 抑制剂，在无细胞试验中IC50为40 nM。同时，也抑制VEGFR3和EGFR，IC50分别为110 nM 和500 nM。对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大，IC50为 1.1-3.6 μM, 对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果，IC50>10 μM。Vandetanib (ZD6474) 可增加凋亡并通过提高 reactive oxygen species (ROS) 的水平来诱导自噬。

  • Lenvatinib (E7080)

    Lenvatinib (E7080)是一种多靶点抑制剂，无细胞试验中，作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效，IC50为4 nM/5.2 nM，对VEGFR1/Flt-1作用效果稍弱，作用于VEGFR2/3比作用于FGFR1， PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、Kit (c-Kit)和RET (c-RET)的抑制剂，并具有强效的抗肿瘤活性。Phase 3。

    Features:E7080是口服有效的多靶点激酶抑制剂。

  • Pazopanib

    Pazopanib (GW786034) 是一种新型多靶点的VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit 和 c-Fms/CSF1R抑制剂，无细胞试验中IC50分别为10 nM，30 nM，47 nM，84 nM，74 nM，140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。

  • Pazopanib HCl (GW786034 HCl)

    Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit和c-fms，在无细胞试验中IC50分别是10 nM，30 nM，47 nM，84 nM，74 nM，140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。

    Features:Pazopanib是一个多激酶的抑制剂。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID