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VEGFR1/2/3FGFR1/2/3PDGFRα/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 购买数量
10mM (1mL in DMSO) RMB 1970.51 现货
RMB 991.25 现货
RMB 5492.96 现货
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

相关VEGFR产品

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VEGFR1/2/3FGFR1/2/3PDGFRα/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)
点击更多
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 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-
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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]

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]
  • 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

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

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
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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,: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: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: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

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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