Elacridar (GF120918)

For research use only. Not for use in humans.

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

Elacridar (GF120918) Chemical Structure

CAS No. 143664-11-3

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

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
有超大折扣

今日订购,明日送达,全国免运费!

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9篇:

客户使用该产品的3个实验数据:

  • Impact of 10 μM elacridar on the intracellular accumulation of 10 μM nintedanib in DMS114 and DMS114/NIN cells was analyzed by confocal fluorescence microscopy after 1 h drug exposure. The scale bar indicates 10 μm.

    J Exp Clin Cancer Res, 2017, 36(1):122. Elacridar (GF120918) purchased from Selleck.

    Effect of drugs on the photo-crosslinking of cysless WT and triple A (Y307A/Q725A/Y953A) mutant P-gp with IAAP. Crude membranes expressing cysless WT or mutant P-gp (60-80 μg protein) were treated with the indicated concentrations of drug in 100 μL buffer containing 50 mM MES-Tris pH 6.8 for 10 min at 37 °C. Samples were then photo-crosslinked with 4–6 nM IAAP at 4 °C as described in Section 2. IAAP-labeling of the cysless WT and Triple A mutant P-gp with no addition of drug was taken as 100% labeling. Both panels show a representative autoradiogram (at the top) and the quantification of the IAAP-labeling (at the bottom). Lane 1, control (DMSO solvent); 2, 1 μM zosuquidar; 3, 1 μM elacridar; and 4, 1 μM tariquidar. Data represent the mean ± the standard deviations for n = 3. Left panel, cysless WT; right panel, Triple A (Y307A/Q725A/Y953A) mutant.

    Biochem Pharmacol, 2016, 101:40-53.. Elacridar (GF120918) purchased from Selleck.

  • Y953A mutant P-gp displays significantly decreased reversal of transport function by zosuquidar, tariquidar and elacridar. The upper panels (A-C) show the histograms for the transport of NBDCsA by the cysless WT and Y953A mutant P-gps. The histograms also show the effect of 50 nM zosuquidar (A), 50 nM tariquidar (B) or 50 nM elacridar (C) on reversal of NBDCsA transport by Y953A mutant P-gp, and by cysless WT P-gp (traces with maximum fluorescence intensity). The lower panels (D–F) show the effect of zosuquidar, tariquidar and elacridar at indicated concentrations on reversal of NBDCsA transport by cysless WT and Y953A mutant P-gp. The transport of NBDCsA in the absence of any inhibitor was taken as 100% for both cysless WT and Y953A mutant, respectively, and the percent of transport in the presence of the different inhibitors was calculated with respect to it. Data points are plotted as the mean + SD (n=3). The values of IC50 (compound concentration that produces 50% inhibition of NBDCsA transport in HeLA cells expressing cysless WT or Y953A mutant P-gp) are given in the figure. The IC50 value of zosuquidar could not be calculated, as a maximum 20% inhibition was observed at the highest concentration. The data was plotted and IC50 values calculated using GraphPad Prism 6.0.

    Biochem Pharmacol, 2016, 101:40-53. Elacridar (GF120918) purchased from Selleck.

产品安全说明书

P-gp抑制剂选择性比较

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 NETO[lZEgXSxdH;4bYNqfHliYYPzZZk> MljhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcZVtfGmmcoXnMZJme2m|dHHueEBUU1[OQkGgZ4VtdHNiaX6gdJJme2WwY3Wgc4Yh[WS{aXHtfYNqdixiSVO1NF0xNjB{zszN NWnUW4g3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG3OVQ3ODJpPkGxO|U1PjB{PD;hQi=>
SKVLB1 MWXDfZRwfG:6aXPpeJkh[XO|YYm= M1\POWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI12dHSrZIL1[{1z\XOrc4ThcpQhW0uYTFKxJINmdGy|LDDJR|UxRTFwNN88US=> Mnm5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF5NUS2NFIoRjFzN{W0OlAzRC:jPh?=
SKOV3 NESyXWZEgXSxdH;4bYNqfHliYYPzZZk> MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whUUN3ME24MlHPxE1? M3;F[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzN{W0OlAzLz5zMUe1OFYxOjxxYU6=
Caco-2 Mof4SpVv[3Srb36gZZN{[Xl? M3jq[2lvcGmkaYTpc44hd2ZiUHfwJI1m[XO3cnXkJIF{KGmwaHnibZRqd25ib3[gX|NJZX[rbnLsZZN1cW6nIHLhd49t[XSncnHsJJRwKGGyaXPhcEB1emGwc4DvdpQhcW5iQ3Hjc{0zKGOnbHzzMEBGSzVyPUNOwG0> NVzOUY5URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUewOlQxPzlpPkG3NFY1ODd7PD;hQi=>
HEK293 Mkj0SpVv[3Srb36gZZN{[Xl? NE\aTpBKdmirYnn0bY9vKG:oIFHCR2czKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNibXn0c5hidnS{b37lMY1m\GmjdHXkJIVn\my3eDDifUBndG:5IHP5eI9u\XS{eTygTWM2OD1yLkSx{txO MlLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MUexPVMoRjF5M{G3NVk{RC:jPh?=
Caco-2 MX7GeY5kfGmxbjDhd5NigQ>? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHBoeCCvZXTpZZRm\CCdM1jdeolv[myjc4TpcoUhfHKjboPwc5J1KGmwIHj1cYFvKEOjY3:tNkBk\WyuczygSWM2OD1{zszN NWHVenhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe5N|Y3OzNpPkG3PVM3PjN|PD;hQi=>
Caco-2 NF7WSmtHfW6ldHnvckBie3OjeR?= NXq5ZW1OUW6qaXLpeIlwdiCxZjDoeY1idiCSLXfsfYNweHKxdHXpckBu\WSrYYTl[EBcO0ifdnnuZoxie3SrbnWgeJJidnOyb4L0JIlvKGi3bXHuJGNi[29vMjDj[YxteyxiRVO1NF0z|ryP MkHuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{NUe1OFUoRjF6MkW3OVQ2RC:jPh?=
Caco-2 NUD3RZBOTnWwY4Tpc44h[XO|YYm= MXTJcohq[mm2aX;uJI9nKGi3bXHuJHAu\3BibXXkbYF1\WRiW{PIYZZqdmKuYYP0bY5mKHS{YX7zdI9zfCCjY4Tpeol1gSCrbjDoeY1idiCFYXPvMVIh[2WubIOsJGVEPTB;Mt88US=> M3;ycVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6Mke2NVQ2Lz5zOEK3OlE1PTxxYU6=
Caco-2 M2XGd2Z2dmO2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKEGEQ1KxMY1m\GmjdHXkJHs{UF24aX7icIF{fGmwZTD0doFve3CxcoTheIlwdiCrbjDoeY1idiCFYXPvMVIh[2WubIOsJGlEPTB;Mt88US=> NHv4Z|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUC1N|g5QCd-MUmwOVM5QDh:L3G+
KBv1 NVixRmhvTnWwY4Tpc44h[XO|YYm= MnrWTY5pcWKrdHnvckBw\iCDQlPCNUBwfmW{ZYjwdoV{e2WmIHnuJIh2dWGwIFvCelEh[2WubIOgZpkh\myxdzDjfZRwdWW2cnnjMYJie2WmIHPhcINmcW5vQV2g[YZndHW6IHHzd4F6NCCLQ{WwQVAvOTl|zszN MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTF5MEWxPUc,OTlzN{C1NVk9N2F-
MCF7/Topo NY\ZeZk6TnWwY4Tpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKEGEQ1eyJI93\XKneIDy[ZN{\WRiaX6gbJVu[W5iTVPGO{9Vd3CxIHPlcIx{KGK7IH\sc5ch[3m2b33leJJq[y2kYYPl[EBucXSxeHHueJJwdmViZX\mcJV5KGG|c3H5MEBKSzVyPUCuNlXPxE1? NFvJNoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG3NFUyQSd-MUmxO|A2OTl:L3G+
MCF7 MX MULGeY5kfGmxbjDhd5NigQ>? NVz5V5E6UW6qaXLpeIlwdiCxZjDCR3JRKGW6cILld5Nm\CCrbjDNR2Y4KE2[IHPlcIx{KGK7IFjv[YNpe3RiM{OzOFIhe3SjaX7pcoctKEmFNUC9NE41|ryP NUXC[pVsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5N|I6PjBpPkG5PVMzQTZyPD;hQi=>
MDCK NIWwe3NHfW6ldHnvckBie3OjeR?= NYT3W|NvUW6qaXLpeIlwdiCxZjDCR3JRKGW6cILld5Nm\CCrbjDNSGNMKGOnbHzzJIJ6KHCqZX;wbI9z[mmmZTDBJIF{e2G7LDDJR|UxRTBwNEROwG0> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl|Mkm2NEc,OTl7M{K5OlA9N2F-
MDCK2-MDR1 MorjSpVv[3Srb36gZZN{[Xl? M162dlYxKG2rboO= NW\UZVZiUW6qaXLpeIlwdiCxZjDoeY1idiCSZ4Cgc5ZmemW6cILld5Nm\CCrbjDoeY1idiCPRFPLNk1OTFJzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWjF{MzDl[oZtfXhiYX\0[ZIhPjBibXnud{whUUN3ME2wMlTPxE1? M2Ha[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEG5OlMzLz5{MUSxPVY{OjxxYU6=
MCF7/Topo NEHWc|JHfW6ldHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKEGEQ1eyJIV5eHKnc4Pl[EBqdiCqdX3hckBOS0Z5L2TvdI8h[2WubIOgZpkhUG:nY3jzeEBucWO{b4DsZZRmKGG|c3H5MEBKSzVyPUCuNVI4|ryP Mn22QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{CyPFIoRjJzNUewNlgzRC:jPh?=
Kb-V1 NFfkN|dHfW6ldHnvckBie3OjeR?= MmDKNVAhdWmwcx?= MY\Jcohq[mm2aX;uJI9nKEGEQ1KxJIV5eHKnc4Pl[EBqdiCNYj3WNUBk\WyuczDh[pRmeiBzMDDtbY5{KGK7IHPhcINmcW5vQV2gZZN{[XluIFnDOVA:OC5zOUROwG0> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5MEK4Nkc,OjF3N{CyPFI9N2F-
Caco2 Mn;aSpVv[3Srb36gZZN{[Xl? Mn75N{B2VQ>? NGDlWFY{OCCvaX7z NHLiNmxKdmirYnn0bY9vKG:oIGCt[5AudWWmaXH0[YQhYzOKXT3kbYdwgGmwIITyZY5{eG:{dDDpckBpfW2jbjDDZYNwOiClZXzsd{BifCB|IIXNJIFnfGW{IEOwJI1qdnN? NXWwOFBJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlY4PzlpPkKyNlY3Pzd7PD;hQi=>
Caco2 MoHNSpVv[3Srb36gZZN{[Xl? Mn;TN{B2VQ>? MnfON|AhdWmwcx?= NIW4OnZKdmirYnn0bY9vKG:oIFLDVnAudWWmaXH0[YQhYzOKXXXzeJJwdmVvMz3zeYxn[XSnIITyZY5{eG:{dDDpckBpfW2jbjDDZYNwOiClZXzsd{BifCB|IIXNJIFnfGW{IEOwJI1qdnN? M{[4ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[2O|c6Lz5{MkK2Olc4QTxxYU6=
CCRF-CEM/VCR1000 NWjOWoxDTnWwY4Tpc44h[XO|YYm= M{\oWWlvcGmkaYTpc44hd2ZiUD3ncJlkd3C{b4TlbY4udWWmaXH0[YQh\GG3bn;yeYJq[2mwIHXm[ox2gCCocn;tJIh2dWGwIFPDVmYuS0WPL2\DVlExODBiY3XscJMh[W[2ZYKgNlQxKHOnY4OgZpkhTkGFUzDmcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OC5yN{K0OO69VQ>? MoLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2NUK0NVIoRjJ{NEWyOFEzRC:jPh?=
MCF7/Topo NGnGR41HfW6ldHnvckBie3OjeR?= NEfHbHEzKGi{cx?= M2fMPGlvcGmkaYTpc44hd2ZiQVLDS|IhcW5iaIXtZY4hVUOINz;Uc5BwKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IFjv[YNpe3RiM{OzOFIhdWmlcn;wcIF1\SCjc4PhfUwhUUN3ME2wMlEzP87:TR?= NGHTe|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY5Oyd-MkS5NFA3QDN:L3G+
KBV1 MWTGeY5kfGmxbjDhd5NigQ>? MlT3NVAhdWmwcx?= NFvUVpZKdmirYnn0bY9vKG:oIFHCR2IyKGmwIHj1cYFvKEuEVkGgZ4VtdHNiYX\0[ZIhOTBibXnud{BjgSCFYXzj[YlvNUGPIH3pZ5JweGyjdHWgZZN{[XluIFnDOVA:OC5zOUROwG0> M2eyTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlg{Lz5{NEmwNFY5OzxxYU6=
A673 MUDxTHRUKGG|c3H5 MVTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MmG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC M2exWpFJXFNiYYPzZZk> NXroeXpSeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NEfVTJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH NXrzU252eUiWUzDhd5NigQ>? MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= MoXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 NYqz[YtLeUiWUzDhd5NigQ>? M2DL[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= M1LXcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
primary glioblastoma stem cells NIDXd5JHfW6ldHnvckBie3OjeR?= NU\RXIJHOTBidH:gNVAxODBibl2= M4rjcFMhcHK| MkPOTY5pcWKrdHnvckBw\iCPRGKxJIlvKGi3bXHuJJBzcW2jcomg[4xqd2KuYYP0c41iKHO2ZX2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hcW62cnHj[YxtfWyjcjDkc5hwenWkaXPpckBi[2O3bYXsZZRqd25iYYSgNVAhfG9iMUCwNFAhdk1iYX\0[ZIhOyCqcoOgZpkhe3CnY4Tyc4ZtfW:{aX3leJJq[yCjbnHsfZNqew>? MoH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3OES4N|goRjNyNUi0PFM5RC:jPh?=
primary mesothelioma stem cells MnrSSpVv[3Srb36gZZN{[Xl? NGfMemsyOCC2bzCxNFAxOCCwTR?= M{nrZVMhcHK| MYnJcohq[mm2aX;uJI9nKE2GUkGgbY4hcHWvYX6gdJJqdWG{eTDt[ZNwfGinbHnvcYEhe3SnbTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBqdnS{YXPlcIx2dGG{IHTvfI9zfWKrY3nuJIFk[3WvdXzheIlwdiCjdDCxNEB1dyBzMECwNEBvVSCjZoTldkA{KGi{czDifUB{eGWldILv[ox2d3KrbXX0dolkKGGwYXz5d4l{ NYPmT3BwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1PFQ5OzhpPkOwOVg1QDN6PD;hQi=>
primary glioblastoma stem cells MmezSpVv[3Srb36gZZN{[Xl? NYK3R3FJOSC3TR?= MoHVO|IhcHK| MVHJcohq[mm2aX;uJI9nKE2GUkGgbY4hcHWvYX6gdJJqdWG{eTDncIlw[myjc4TvcYEhe3SnbTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBld3ixcoXibYNqdi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjdDCxJJVOKGGodHXyJFczKGi{czDifUBCXFCuaYTlJIx2dWmwZYPj[Y5k\SCjc4PhfS=> M{XJd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUi0PFM5Lz5|MEW4OFg{QDxxYU6=
primary mesothelioma stem cells NV7Kd5puTnWwY4Tpc44h[XO|YYm= MUKxJJVO NGiyTnE4OiCqcoO= NIrLdHlKdmirYnn0bY9vKG:oIF3EVlEhcW5iaIXtZY4heHKrbXHyfUBu\XOxdHjlcIlwdWFic4TlcUBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCmb4jvdpVjcWOrbj3pcoR2[2WmIILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDheEAyKHWPIHHmeIVzKDd{IHjyd{BjgSCDVGDsbZRmKGy3bXnu[ZNk\W6lZTDhd5NigQ>? NV7YS2xNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1PFQ5OzhpPkOwOVg1QDN6PD;hQi=>
primary glioblastoma stem cells NWi4TolVTnWwY4Tpc44h[XO|YYm= M1LpZVEhfU1? NUjNPWRzOjRiaILz NWSyTXZ4UW6qaXLpeIlwdiCxZjDNSHIyKGmwIHj1cYFvKHC{aX3hdpkh\2yrb3LsZZN1d22jIIP0[Y0h[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iZH;4c5J2[mmlaX6tbY5lfWOnZDDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZZQhOSC3TTDh[pRmeiB{NDDodpMh[nliYomgUGRJKHKnbHXhd4Uh[XO|YYm= NY\tSFZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1PFQ5OzhpPkOwOVg1QDN6PD;hQi=>
primary mesothelioma stem cells NGnDeHpHfW6ldHnvckBie3OjeR?= NYXvbJVUOSC3TR?= NHKyOIQzPCCqcoO= M3X0ZmlvcGmkaYTpc44hd2ZiTVTSNUBqdiCqdX3hckBxemmvYYL5JI1me2:2aHXsbY9u[SC|dHXtJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGSxeH;yeYJq[2mwLXnu[JVk\WRicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHH0JFEhfU1iYX\0[ZIhOjRiaILzJIJ6KGK7IFzETEBz\WynYYPlJIF{e2G7 Mn7WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3OES4N|goRjNyNUi0PFM5RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability ; 

PubMed: 25862759     


IC50 curve of GL261 glioma cells with elacridar (ELD). IC50=5.8 μM

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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验:[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 8 mg/mL warmed (14.19 mM)
Water Insoluble
Ethanol 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):
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 粉状
溶于溶剂
别名 GW120918, GG918, GW0918

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
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

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

P-gp Signaling Pathway Map

相关P-gp产品

Tags: 购买Elacridar (GF120918) | Elacridar (GF120918)供应商 | 采购Elacridar (GF120918) | Elacridar (GF120918)价格 | Elacridar (GF120918)生产 | 订购Elacridar (GF120918) | Elacridar (GF120918)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID