Elacridar (GF120918)

目录号:S7772 别名: GW120918, GG918, GW0918 中文名称:依克立达

仅限科研使用

Elacridar (GF120918, GW120918, GG918, GW0918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。

Elacridar (GF120918) Chemical Structure

CAS: 143664-11-3

规格 价格 库存 购买数量
RMB 811.44 现货
RMB 2439.78 现货
RMB 6519.55 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Elacridar (GF120918)发表文献11篇:

客户使用该产品的3个实验数据:

产品安全说明书

P-gp抑制剂选择性比较

相关P-gp产品

生物活性

产品描述 Elacridar (GF120918, GW120918, GG918, GW0918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。
靶点
P-gp [1] BCRP [1]
体外研究

Elacridar 抑制[3H]azidopine对P糖蛋白的标记,IC50值为0.16μM。[2] 在Caki-1和 ACHN细胞中,elacridar (2.5 μM)显著抑制细胞生长。Elacridar能够抑制P糖蛋白的活性。Elacridar 和sunitinib的联合使用显著降低ABC亚家族B分子2(ABCG2) 在786-O细胞中的表达。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKVLB1 NXjEc3p6S3m2b4TvfIlkcXS7IHHzd4F6 NX\rdZVIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdXWudHnkdpVoNXKnc3nzeIFvfCCVS2\MRlEh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiYXTybYFugWOrbjygTWM2OD1yLkCy{txO MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTd3NE[wNkc,OTF5NUS2NFI9N2F-
SKVLB1 MYrDfZRwfG:6aXPpeJkh[XO|YYm= MkLsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcZVtfGmmcoXnMZJme2m|dHHueEBUU1[OQkGgZ4VtdHNuIFnDOVA:OS52zszN MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTd3NE[wNkc,OTF5NUS2NFI9N2F-
SKOV3 MWPDfZRwfG:6aXPpeJkh[XO|YYm= NXTKU3lFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNuIFnDOVA:QC5zzszN NVfzOoFKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG3OVQ3ODJpPkGxO|U1PjB{PD;hQi=>
Caco-2 NXrhUFB1TnWwY4Tpc44h[XO|YYm= NVTKWmZ3UW6qaXLpeIlwdiCxZjDQ[5AhdWWjc4Xy[YQh[XNiaX7obYJqfGmxbjDv[kBcO0ifdnnuZoxie3SrbnWgZoF{d2yjdHXyZYwhfG9iYYDpZ4FtKHS{YX7zdI9zfCCrbjDDZYNwNTJiY3XscJMtKEWFNUC9Nu69VQ>? NVu0NpU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUewOlQxPzlpPkG3NFY1ODd7PD;hQi=>
HEK293 MkL0SpVv[3Srb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKEGEQ1eyJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMhdWm2b4jhcpRzd26nLX3l[IlifGWmIHXm[ox2gCCkeTDmcI94KGO7dH;t[ZRzgSxiSVO1NF0xNjRzzszN NEfoWm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OxO|E6Oyd-MUezNVcyQTN:L3G+
Caco-2 NWrGXHJ[TnWwY4Tpc44h[XO|YYm= Mkn4TY5pcWKrdHnvckBw\iCqdX3hckBR\3BibXXkbYF1\WRiW{PIYZZqdmKuYYP0bY5mKHS{YX7zdI9zfCCrbjDoeY1idiCFYXPvMVIh[2WubIOsJGVEPTB;Mt88US=> MmHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7M{[2N|MoRjF5OUO2OlM{RC:jPh?=
Caco-2 M1rn[WZ2dmO2aX;uJIF{e2G7 NUXxUYs1UW6qaXLpeIlwdiCxZjDoeY1idiCSLXfsfYNweHKxdHXpckBu\WSrYYTl[EBcO0ifdnnuZoxie3SrbnWgeJJidnOyb4L0JIlvKGi3bXHuJGNi[29vMjDj[YxteyxiRVO1NF0z|ryP NIi0UYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEK1O|U1PSd-MUiyOVc2PDV:L3G+
Caco-2 NInwZYVHfW6ldHnvckBie3OjeR?= NWXYW2E4UW6qaXLpeIlwdiCxZjDoeY1idiCSLXfwJI1m\GmjdHXkJHs{UF24aX7icIF{fGmwZTD0doFve3CxcoSgZYN1cX[rdImgbY4hcHWvYX6gR4Fkdy1{IHPlcIx{NCCHQ{WwQVLPxE1? NHXOblk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEK3OlE1PSd-MUiyO|YyPDV:L3G+
Caco-2 NWnXTGo4TnWwY4Tpc44h[XO|YYm= NWXNd2pGUW6qaXLpeIlwdiCxZjDBRmNDOS2vZXTpZZRm\CCdM1jdeolv[myjc4TpcoUhfHKjboPwc5J1[XSrb36gbY4hcHWvYX6gR4Fkdy1{IHPlcIx{NCCLQ{WwQVLPxE1? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTB3M{i4PEc,OTlyNUO4PFg9N2F-
KBv1 M1vqPWZ2dmO2aX;uJIF{e2G7 M4jFbGlvcGmkaYTpc44hd2ZiQVLDRlEhd3[ncnX4dJJme3OnZDDpckBpfW2jbjDLRpYyKGOnbHzzJIJ6KG[ub4egZ5l1d22ndILpZ{1j[XOnZDDjZYxk\WmwLVHNJIVn\my3eDDhd5NigSxiSVO1NF0xNjF7M988US=> Mm\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzN{C1NVkoRjF7MUewOVE6RC:jPh?=
MCF7/Topo M{LGd2Z2dmO2aX;uJIF{e2G7 MWPJcohq[mm2aX;uJI9nKEGEQ1eyJI93\XKneIDy[ZN{\WRiaX6gbJVu[W5iTVPGO{9Vd3CxIHPlcIx{KGK7IH\sc5ch[3m2b33leJJq[y2kYYPl[EBucXSxeHHueJJwdmViZX\mcJV5KGG|c3H5MEBKSzVyPUCuNlXPxE1? NUDhZpF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxO|A2OTlpPkG5NVcxPTF7PD;hQi=>
MCF7 MX M3S1TWZ2dmO2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJIlvKE2FRkegUXgh[2WubIOgZpkhUG:nY3jzeEA{OzN2MjDzeIFqdmmwZzygTWM2OD1yLkVOwG0> NVfu[4kxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5N|I6PjBpPkG5PVMzQTZyPD;hQi=>
MDCK MmjwSpVv[3Srb36gZZN{[Xl? M3n5bWlvcGmkaYTpc44hd2ZiQlPSVEBmgHC{ZYPz[YQhcW5iTVTDT{Bk\WyuczDifUBxcGWxcHjvdoJq\GViQTDhd5NigSxiSVO1NF0xNjR|zszN NG\Ic5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmzNlk3OCd-MUm5N|I6PjB:L3G+
MDCK2-MDR1 M4fCV2Z2dmO2aX;uJIF{e2G7 MlvNOlAhdWmwcx?= NF3RTHhKdmirYnn0bY9vKG:oIHj1cYFvKFCpcDDveoVz\XiycnXzd4VlKGmwIHj1cYFvKE2GQ1uyMW1FWjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBTOTJ|IHXm[ox2gCCjZoTldkA3OCCvaX7zMEBKSzVyPUCuOO69VQ>? M1WzSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEG5OlMzLz5{MUSxPVY{OjxxYU6=
MCF7/Topo NGrHdFFHfW6ldHnvckBie3OjeR?= NHTBfYxKdmirYnn0bY9vKG:oIFHCR2czKGW6cILld5Nm\CCrbjDoeY1idiCPQ1[3M3RweG9iY3XscJMh[nliSH;lZ4h{fCCvaXPyc5Bt[XSnIHHzd4F6NCCLQ{WwQVAvOTJ5zszN MoHQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{CyPFIoRjJzNUewNlgzRC:jPh?=
Kb-V1 NWDuempKTnWwY4Tpc44h[XO|YYm= MoDtNVAhdWmwcx?= M1nDNGlvcGmkaYTpc44hd2ZiQVLDRlEh\XiycnXzd4VlKGmwIFviMXYyKGOnbHzzJIFnfGW{IEGwJI1qdnNiYomgZ4Ft[2Wrbj3BUUBie3OjeTygTWM2OD1yLkG5N:69VQ>? NYLDXI9MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|AzQDJpPkKxOVcxOjh{PD;hQi=>
Caco2 NGHjXZdHfW6ldHnvckBie3OjeR?= Moj2N{B2VQ>? NVW3SlRwOzBibXnudy=> MoP4TY5pcWKrdHnvckBw\iCSLXfwMY1m\GmjdHXkJHs{UF1vZHnnc5hqdiC2cnHud5BwenRiaX6gbJVu[W5iQ3Hjc|Ih[2WubIOgZZQhOyC3TTDh[pRmeiB|MDDtbY5{ Ml;ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{Nk[3O|koRjJ{Mk[2O|c6RC:jPh?=
Caco2 NEHVVXdHfW6ldHnvckBie3OjeR?= NYjNc4c2OyC3TR?= NVrCbG4{OzBibXnudy=> M{nQ[mlvcGmkaYTpc44hd2ZiQlPSVE1u\WSrYYTl[EBcO0ifZYP0do9v\S1|LYP1cIZifGVidILhcpNxd3K2IHnuJIh2dWGwIFPhZ48zKGOnbHzzJIF1KDNidV2gZYZ1\XJiM{CgcYlvew>? MoLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{Nk[3O|koRjJ{Mk[2O|c6RC:jPh?=
CCRF-CEM/VCR1000 MU\GeY5kfGmxbjDhd5NigQ>? NHHmNpVKdmirYnn0bY9vKG:oIGCt[4x6[2:ycn;0[YlvNW2nZHnheIVlKGSjdX7vdpVjcWOrbjDl[oZtfXhiZoLvcUBpfW2jbjDDR3JHNUOHTT;WR3IyODByIHPlcIx{KGGodHXyJFI1OCC|ZXPzJIJ6KE[DQ2Og[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTBwMEeyOFTPxE1? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR3MkSxNkc,OjJ2NUK0NVI9N2F-
MCF7/Topo NXLDTpJFTnWwY4Tpc44h[XO|YYm= MYeyJIhzew>? MUfJcohq[mm2aX;uJI9nKEGEQ1eyJIlvKGi3bXHuJG1ETjdxVH;wc{Bk\WyuczDh[pRmeiB{IHjyd{BjgSCKb3XjbJN1KDN|M{SyJI1q[3KxcHzheIUh[XO|YYmsJGlEPTB;MD6xNlfPxE1? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[4N{c,OjR7MEC2PFM9N2F-
KBV1 M2iyUWZ2dmO2aX;uJIF{e2G7 NULWR2d{OTBibXnudy=> MoO3TY5pcWKrdHnvckBw\iCDQlPCNUBqdiCqdX3hckBMSlZzIHPlcIx{KGGodHXyJFExKG2rboOgZpkhS2GuY3Xpck1CVSCvaXPyc5Bt[XSnIHHzd4F6NCCLQ{WwQVAvOTl|zszN MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[4N{c,OjR7MEC2PFM9N2F-
A673 MkPMdWhVWyCjc4PhfS=> MmS3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NIjVepFyUFSVIHHzd4F6 NFPnNHJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M3uwO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH NHnocoJyUFSVIHHzd4F6 NUPhTGJ5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> NXLoWXlNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NX;afFRReUiWUzDhd5NigQ>? MoXFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MlH1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
primary glioblastoma stem cells MoDDSpVv[3Srb36gZZN{[Xl? NF7E[pkyOCC2bzCxNFAxOCCwTR?= M{HWXVMhcHK| NHi5OIlKdmirYnn0bY9vKG:oIF3EVlEhcW5iaIXtZY4heHKrbXHyfUBodGmxYnzhd5RwdWFic4TlcUBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJIRwgG:{dXLpZ4lvKGGlY4XteYxifGmxbjDheEAyOCC2bzCxNFAxOCCwTTDh[pRmeiB|IHjyd{BjgSC|cHXjeJJw\my3b4LpcYV1emmlIHHuZYx6e2m| NIXxXHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEW4OFg{QCd-M{C1PFQ5Ozh:L3G+
primary mesothelioma stem cells MnzwSpVv[3Srb36gZZN{[Xl? NYKxPWVqOTBidH:gNVAxODBibl2= MkHCN{BpenN? MVPJcohq[mm2aX;uJI9nKE2GUkGgbY4hcHWvYX6gdJJqdWG{eTDt[ZNwfGinbHnvcYEhe3SnbTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBqdnS{YXPlcIx2dGG{IHTvfI9zfWKrY3nuJIFk[3WvdXzheIlwdiCjdDCxNEB1dyBzMECwNEBvVSCjZoTldkA{KGi{czDifUB{eGWldILv[ox2d3KrbXX0dolkKGGwYXz5d4l{ M4\hdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUi0PFM5Lz5|MEW4OFg{QDxxYU6=
primary glioblastoma stem cells MUnGeY5kfGmxbjDhd5NigQ>? MXexJJVO MV23NkBpenN? MUTJcohq[mm2aX;uJI9nKE2GUkGgbY4hcHWvYX6gdJJqdWG{eTDncIlw[myjc4TvcYEhe3SnbTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBld3ixcoXibYNqdi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjdDCxJJVOKGGodHXyJFczKGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfS=> MkXKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3OES4N|goRjNyNUi0PFM5RC:jPh?=
primary mesothelioma stem cells NEjlfpFHfW6ldHnvckBie3OjeR?= NVv4VYtFOSC3TR?= NYr5THRIPzJiaILz MmTOTY5pcWKrdHnvckBw\iCPRGKxJIlvKGi3bXHuJJBzcW2jcomgcYV{d3SqZXzpc41iKHO2ZX2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h\G:6b4L1ZolkcW5vaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYYSgNUB2VSCjZoTldkA4OiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZk> NYDFcVlkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1PFQ5OzhpPkOwOVg1QDN6PD;hQi=>
primary glioblastoma stem cells MVvGeY5kfGmxbjDhd5NigQ>? M{iycFEhfU1? MWqyOEBpenN? MnPmTY5pcWKrdHnvckBw\iCPRGKxJIlvKGi3bXHuJJBzcW2jcomg[4xqd2KuYYP0c41iKHO2ZX2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h\G:6b4L1ZolkcW5vaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYYSgNUB2VSCjZoTldkAzPCCqcoOgZpkh[nliTFTIJJJmdGWjc3WgZZN{[Xl? NV;ITnRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1PFQ5OzhpPkOwOVg1QDN6PD;hQi=>
primary mesothelioma stem cells NWrNPI05TnWwY4Tpc44h[XO|YYm= MmC2NUB2VQ>? M{PJXVI1KGi{cx?= M3yydWlvcGmkaYTpc44hd2ZiTVTSNUBqdiCqdX3hckBxemmvYYL5JI1me2:2aHXsbY9u[SC|dHXtJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGSxeH;yeYJq[2mwLXnu[JVk\WRicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHH0JFEhfU1iYX\0[ZIhOjRiaILzJIJ6KGK7IFzETEBz\WynYYPlJIF{e2G7 NHuxNYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEW4OFg{QCd-M{C1PFQ5Ozh:L3G+
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 25862759
体内研究 在野生型小鼠中, elacridar (100 毫克/千克,腹腔注射) 和crizotinib口服联合给药,增加血浆和脑组织中crizotinib的浓度,和crizotinib的大脑-血浆比值,与Abcb1a/1b; Abcg2-/-小鼠体内水平相当。[1] 在弗兰德白血病病毒染色的B模型小鼠中,elacridar静脉注射(2.5 毫克/千克),腹腔注射(100毫克/千克)和口服 (100毫克/千克)后,大脑-血浆中的分配系数(Kp,大脑)分别为0.82, 0.43和 4.31。[4] 在Mrp4(-/-) 模型小鼠中,elacridar充分抑制P糖蛋白介导的topotecan转运,但是对Bcrp1介导的转运抑制效果有限。[5]

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:[2]
  • P-gp 的光亲和性放射性标记:

    10 微升未标记的细胞膜悬液(蛋白量0.4 毫克/毫升)等分加入到96孔板中。然后每孔加5 微升GF120918。板在25℃下避光培养25 分钟。每孔加5 微升氚标记的azidopine(1.8 TBq/mmol)(0.6 μM in HCI 0.2 mM)。25℃下避光培养25 分钟后,用薄层色谱法设计的UV紫外灯直接与板接触,0℃下,254 nm 光照样品2 分钟。用十二烷基硫酸钠聚丙烯酰胺凝胶电泳的上样缓冲液溶解样品,但不加热。7.5%聚丙烯酰胺凝胶电泳分离后,凝胶经荧光放大处理,感光胶片曝光3天。用Camag薄层色谱扫描仪II密度计分析荧光显影。

细胞实验:[3]
  • Cell lines: ACHN,Caki-1,786-O,和 MCF-7 细胞
  • Concentrations: ~ 5 mM
  • Incubation Time: 48小时
  • Method: 以3000个细胞/孔的密度接种至96孔板中。培养24 小时后,将适宜浓度梯度的elacridar加至孔中。培养48 小时后,使用增殖试剂,MTT检测细胞活性。对照组细胞用载体(1% DMSO)处理。最终培育后,抽出培养基,沉淀的甲瓒晶体溶解在DMSO (100 微升/孔)中。每孔的吸光度在540 nm下测量,以650 nm为参比波长,在multiskan JX酶标仪上读取数据。细胞活性以对照组值的百分比计算。
动物实验:[1]
  • Animal Models: 雄性野生型,Abcb1a/1b-/-34,Abcg2 -/-32 和 Abcb1a/1b;Abcg2
  • Dosages: 100 毫克/千克
  • Administration: 口服

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):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O

1mg/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 563.64
化学式

C34H33N3O5

CAS号 143664-11-3
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

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