Elacridar (GF120918)

Catalog No.S7772 Synonyms: GW120918, GG918, GW0918

For research use only.

Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.

Elacridar (GF120918) Chemical Structure

CAS No. 143664-11-3

Selleck's Elacridar (GF120918) has been cited by 11 Publications

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Biological Activity

Description Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Targets
P-gp [1] BCRP [1]
In vitro

Elacridar inhibits P-glycoprotein (P-gp) labeling by [3H]azidopine with a IC50 of 0.16 μM. [2] In Caki-1 and ACHN cells, elacridar ( 2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by elacridar. The combination of elacridar and sunitinib lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKVLB1 MWnDfZRwfG:6aXPpeJkh[XO|YYm= NHPyfmhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBufWy2aXTyeYcuemW|aYP0ZY51KFONVlzCNUBk\WyuczDpckBxemW|ZX7j[UBw\iCjZILpZY16[2mwLDDJR|UxRTBwMENOwG0> NEnaWWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUe1OFYxOid-MUG3OVQ3ODJ:L3G+
SKVLB1 M4[zNWN6fG:2b4jpZ4l1gSCjc4PhfS=> MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDteYx1cWS{dXetdoV{cXO2YX70JHNMXkyEMTDj[YxteyxiSVO1NF0yNjUQvF2= M1PDWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzN{W0OlAzLz5zMUe1OFYxOjxxYU6=
SKOV3 NWfUSGxiS3m2b4TvfIlkcXS7IHHzd4F6 M1f3PGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{NCCLQ{WwQVgvOc7:TR?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTd3NE[wNkc,OTF5NUS2NFI9N2F-
Caco-2 NYjmcZNkTnWwY4Tpc44h[XO|YYm= MmfOTY5pcWKrdHnvckBw\iCSZ4CgcYVie3W{ZXSgZZMhcW6qaXLpeIlwdiCxZjDbN2hefmmwYnzhd5RqdmViYnHzc4xifGW{YXygeI8h[XCrY3HsJJRz[W6|cH;yeEBqdiCFYXPvMVIh[2WubIOsJGVEPTB;Mt88US=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzB4NEC3PUc,OTdyNkSwO|k9N2F-
HEK293 NYrNR40yTnWwY4Tpc44h[XO|YYm= M3POOGlvcGmkaYTpc44hd2ZiQVLDS|Ih\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bie3Onc4Pl[EBieyCvaYTvfIFvfHKxbnWtcYVlcWG2ZXSg[YZndHW6IHL5JIZtd3diY4n0c41mfHK7LDDJR|UxRTBwNEJOwG0> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNzN{G5N{c,OTd|MUexPVM9N2F-
Caco-2 NF;vfnlHfW6ldHnvckBie3OjeR?= M4jtc2lvcGmkaYTpc44hd2ZiaIXtZY4hWGeyIH3l[IlifGWmIGuzTH13cW6kbHHzeIlv\SC2cnHud5BwenRiaX6gbJVu[W5iQ3Hjc{0zKGOnbHzzMEBGSzVyPUNOwG0> NI\qZVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{mzOlY{Oyd-MUe5N|Y3OzN:L3G+
Caco-2 NGrj[JNHfW6ldHnvckBie3OjeR?= NGWxWYJKdmirYnn0bY9vKG:oIHj1cYFvKFBvZ3z5Z49xem:2ZXnuJI1m\GmjdHXkJHs{UF24aX7icIF{fGmwZTD0doFve3CxcoSgbY4hcHWvYX6gR4Fkdy1{IHPlcIx{NCCHQ{WwQVLPxE1? M3nSbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkW3OVQ2Lz5zOEK1O|U1PTxxYU6=
Caco-2 NHjnOHBHfW6ldHnvckBie3OjeR?= NVj6N4xVUW6qaXLpeIlwdiCxZjDoeY1idiCSLXfwJI1m\GmjdHXkJHs{UF24aX7icIF{fGmwZTD0doFve3CxcoSgZYN1cX[rdImgbY4hcHWvYX6gR4Fkdy1{IHPlcIx{NCCHQ{WwQVLPxE1? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ5NkG0OUc,OTh{N{[xOFU9N2F-
Caco-2 NFTYTZBHfW6ldHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKEGEQ1KxMY1m\GmjdHXkJHs{UF24aX7icIF{fGmwZTD0doFve3CxcoTheIlwdiCrbjDoeY1idiCFYXPvMVIh[2WubIOsJGlEPTB;Mt88US=> NEDRVZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUC1N|g5QCd-MUmwOVM5QDh:L3G+
KBv1 MkXRSpVv[3Srb36gZZN{[Xl? NXvmemJFUW6qaXLpeIlwdiCxZjDBRmNDOSCxdnXy[ZhxemW|c3XkJIlvKGi3bXHuJGtDfjFiY3XscJMh[nliZnzve{BkgXSxbXX0dolkNWKjc3XkJINidGOnaX6tRW0h\W[obIX4JIF{e2G7LDDJR|UxRTBwMUmz{txO M2fQV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MUewOVE6Lz5zOUG3NFUyQTxxYU6=
MCF7/Topo Mnr6SpVv[3Srb36gZZN{[Xl? MoHDTY5pcWKrdHnvckBw\iCDQlPHNkBwfmW{ZYjwdoV{e2WmIHnuJIh2dWGwIF3DSlcwXG:ybzDj[YxteyCkeTDmcI94KGO7dH;t[ZRzcWNvYnHz[YQhdWm2b4jhcpRzd26nIHXm[ox2gCCjc4PhfUwhUUN3ME2wMlI2|ryP MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTF5MEWxPUc,OTlzN{C1NVk9N2F-
MCF7 MX MX3GeY5kfGmxbjDhd5NigQ>? MWrJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJIlvKE2FRkegUXgh[2WubIOgZpkhUG:nY3jzeEA{OzN2MjDzeIFqdmmwZzygTWM2OD1yLkVOwG0> M3\XUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUOyPVYxLz5zOUmzNlk3ODxxYU6=
MDCK NIO1[YJHfW6ldHnvckBie3OjeR?= NUnCUW5EUW6qaXLpeIlwdiCxZjDCR3JRKGW6cILld5Nm\CCrbjDNSGNMKGOnbHzzJIJ6KHCqZX;wbI9z[mmmZTDBJIF{e2G7LDDJR|UxRTBwNEROwG0> NE\hRZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmzNlk3OCd-MUm5N|I6PjB:L3G+
MDCK2-MDR1 M1zGUWZ2dmO2aX;uJIF{e2G7 NVfMe5VpPjBibXnudy=> NWniV4EzUW6qaXLpeIlwdiCxZjDoeY1idiCSZ4Cgc5ZmemW6cILld5Nm\CCrbjDoeY1idiCPRFPLNk1OTFJzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWjF{MzDl[oZtfXhiYX\0[ZIhPjBibXnud{whUUN3ME2wMlTPxE1? NYnBUI9FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0NVk3OzJpPkKxOFE6PjN{PD;hQi=>
MCF7/Topo MVfGeY5kfGmxbjDhd5NigQ>? MXvJcohq[mm2aX;uJI9nKEGEQ1eyJIV5eHKnc4Pl[EBqdiCqdX3hckBOS0Z5L2TvdI8h[2WubIOgZpkhUG:nY3jzeEBucWO{b4DsZZRmKGG|c3H5MEBKSzVyPUCuNVI4|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5MEK4Nkc,OjF3N{CyPFI9N2F-
Kb-V1 M1vnZWZ2dmO2aX;uJIF{e2G7 NYXXT2RDOTBibXnudy=> MmrZTY5pcWKrdHnvckBw\iCDQlPCNUBmgHC{ZYPz[YQhcW5iS3KtWlEh[2WubIOgZYZ1\XJiMUCgcYlveyCkeTDjZYxk\WmwLVHNJIF{e2G7LDDJR|UxRTBwMUmz{txO MojZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{CyPFIoRjJzNUewNlgzRC:jPh?=
Caco2 MoS0SpVv[3Srb36gZZN{[Xl? M3zKNlMhfU1? NY\JelVGOzBibXnudy=> NFPZRnRKdmirYnn0bY9vKG:oIGCt[5AudWWmaXH0[YQhYzOKXT3kbYdwgGmwIITyZY5{eG:{dDDpckBpfW2jbjDDZYNwOiClZXzsd{BifCB|IIXNJIFnfGW{IEOwJI1qdnN? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Nke3PUc,OjJ{Nk[3O|k9N2F-
Caco2 NVy1U2d1TnWwY4Tpc44h[XO|YYm= MV:zJJVO Mlf0N|AhdWmwcx?= MYnJcohq[mm2aX;uJI9nKEKFUmCtcYVlcWG2ZXSgX|NJZWW|dILvcoUuOy2|dXzmZZRmKHS{YX7zdI9zfCCrbjDoeY1idiCFYXPvNkBk\WyuczDheEA{KHWPIHHmeIVzKDNyIH3pcpM> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Nke3PUc,OjJ{Nk[3O|k9N2F-
CCRF-CEM/VCR1000 M2fiNWZ2dmO2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMY1m\GmjdHXkJIRifW6xcoXibYNqdiCnZn\seZgh\nKxbTDoeY1idiCFQ2LGMWNGVS:YQ2KxNFAxKGOnbHzzJIFnfGW{IEK0NEB{\WO|IHL5JGZCS1NiZnzve{BkgXSxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVAvODd{NEVOwG0> MlPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2NUK0NVIoRjJ{NEWyOFEzRC:jPh?=
MCF7/Topo Mn3jSpVv[3Srb36gZZN{[Xl? MoDiNkBpenN? MXXJcohq[mm2aX;uJI9nKEGEQ1eyJIlvKGi3bXHuJG1ETjdxVH;wc{Bk\WyuczDh[pRmeiB{IHjyd{BjgSCKb3XjbJN1KDN|M{SyJI1q[3KxcHzheIUh[XO|YYmsJGlEPTB;MD6xNlfPxE1? NITs[Fc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY5Oyd-MkS5NFA3QDN:L3G+
KBV1 M{Pzd2Z2dmO2aX;uJIF{e2G7 M2fOTlExKG2rboO= NUjhSo1[UW6qaXLpeIlwdiCxZjDBRmNDOSCrbjDoeY1idiCNQm[xJINmdGy|IHHmeIVzKDFyIH3pcpMh[nliQ3HsZ4Vqdi2DTTDtbYNzd3CuYYTlJIF{e2G7LDDJR|UxRTBwMUmz{txO MoC4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2PFMoRjJ2OUCwOlg{RC:jPh?=
A673 NInscWxyUFSVIHHzd4F6 MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NFS0UJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NGXrNnhyUFSVIHHzd4F6 MonGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M1LHNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH NE[xepByUFSVIHHzd4F6 MmHvdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 M{fwbJFJXFNiYYPzZZk> MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| M4e5eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
primary glioblastoma stem cells NY[0bYd1TnWwY4Tpc44h[XO|YYm= NWfKV3RnOTBidH:gNVAxODBibl2= NVe1V4pDOyCqcoO= MnLmTY5pcWKrdHnvckBw\iCPRGKxJIlvKGi3bXHuJJBzcW2jcomg[4xqd2KuYYP0c41iKHO2ZX2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hcW62cnHj[YxtfWyjcjDkc5hwenWkaXPpckBi[2O3bYXsZZRqd25iYYSgNVAhfG9iMUCwNFAhdk1iYX\0[ZIhOyCqcoOgZpkhe3CnY4Tyc4ZtfW:{aX3leJJq[yCjbnHsfZNqew>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODV6NEizPEc,OzB3OES4N|g9N2F-
primary mesothelioma stem cells NIjJVIxHfW6ldHnvckBie3OjeR?= MYWxNEB1dyBzMECwNEBvVQ>? NESzd4o{KGi{cx?= MkDGTY5pcWKrdHnvckBw\iCPRGKxJIlvKGi3bXHuJJBzcW2jcomgcYV{d3SqZXzpc41iKHO2ZX2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hcW62cnHj[YxtfWyjcjDkc5hwenWkaXPpckBi[2O3bYXsZZRqd25iYYSgNVAhfG9iMUCwNFAhdk1iYX\0[ZIhOyCqcoOgZpkhe3CnY4Tyc4ZtfW:{aX3leJJq[yCjbnHsfZNqew>? NXW1UpBnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1PFQ5OzhpPkOwOVg1QDN6PD;hQi=>
primary glioblastoma stem cells MmfwSpVv[3Srb36gZZN{[Xl? NUWwWlZKOSC3TR?= Mo\MO|IhcHK| MmG3TY5pcWKrdHnvckBw\iCPRGKxJIlvKGi3bXHuJJBzcW2jcomg[4xqd2KuYYP0c41iKHO2ZX2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h\G:6b4L1ZolkcW5vaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYYSgNUB2VSCjZoTldkA4OiCqcoOgZpkhSVSSbHn0[UBtfW2rbnXzZ4Vv[2ViYYPzZZk> M3e1[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUi0PFM5Lz5|MEW4OFg{QDxxYU6=
primary mesothelioma stem cells NXnWcnZDTnWwY4Tpc44h[XO|YYm= M13NUFEhfU1? M4LEWlczKGi{cx?= NX3MUW45UW6qaXLpeIlwdiCxZjDNSHIyKGmwIHj1cYFvKHC{aX3hdpkhdWW|b4To[Yxqd22jIIP0[Y0h[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iZH;4c5J2[mmlaX6tbY5lfWOnZDDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZZQhOSC3TTDh[pRmeiB5MjDodpMh[nliQWTQcIl1\SCudX3pcoV{[2WwY3WgZZN{[Xl? M3PSe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUi0PFM5Lz5|MEW4OFg{QDxxYU6=
primary glioblastoma stem cells NHO1[JdHfW6ldHnvckBie3OjeR?= M1nkfFEhfU1? M{\N[lI1KGi{cx?= MkPZTY5pcWKrdHnvckBw\iCPRGKxJIlvKGi3bXHuJJBzcW2jcomg[4xqd2KuYYP0c41iKHO2ZX2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h\G:6b4L1ZolkcW5vaX7keYNm\CC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYYSgNUB2VSCjZoTldkAzPCCqcoOgZpkh[nliTFTIJJJmdGWjc3WgZZN{[Xl? M4DjSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUi0PFM5Lz5|MEW4OFg{QDxxYU6=
primary mesothelioma stem cells Mk\SSpVv[3Srb36gZZN{[Xl? MWCxJJVO M2jtS|I1KGi{cx?= NVLPOFdtUW6qaXLpeIlwdiCxZjDNSHIyKGmwIHj1cYFvKHC{aX3hdpkhdWW|b4To[Yxqd22jIIP0[Y0h[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iZH;4c5J2[mmlaX6tbY5lfWOnZDDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZZQhOSC3TTDh[pRmeiB{NDDodpMh[nliYomgUGRJKHKnbHXhd4Uh[XO|YYm= MmrwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3OES4N|goRjNyNUi0PFM5RC:jPh?=
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 25862759
In vivo Oral co-administration of elacridar (100 mg/kg, p.o.) and crizotinib increases the plasma and brain concentrations and brain-to-plasma ratios of crizotinib in wild-type mice, equaling the levels in Abcb1a/1b; Abcg2-/- mice. [1] In friend leukemia virus stain B mice, the brain-to-plasm partition coefficient (Kp, brain) of elacridar is 0.82, 0.43, and 4.31 after intravenous (2.5 mg/kg), intraperitoneal (100 mg/kg), and oral (100 mg/kg) treatment, respectively. [4] In Mrp4(-/-) mice, elacridar fully inhibits P-gp mediated transport of topotecan, without siginificant effects on Bcrp1-mediated transport. [5]

Protocol (from reference)

Kinase Assay:[2]
  • Photoaffinity radiolabeling of P-gp:

    10 μL of unlabeled cell membrane suspension (at 0.4 mg of protein/mL) are aliquoted into each well in 96-well plates. 5 μL of GF120918 are then added to each well. The plate is incubated 25 min at 25℃ in the dark. 5 μL of tritiated azidopine (1.8 TBq/mmol) (0.6 μM in HCI 0.2 mM) are added to each well. After 25 min of incubation at 25℃ in the dark, samples are simultaneously irradiated for 2 min at 254 nm at 0℃ with a thin layer chromatography-designed UV lamp directly in contact with the plate. Samples are solubilized in sodium dodecyl sulfate-polyacrylamide gel electrophoresis sample buffer but not heated. After separation on a 7.5% polyacrylamide gel, the gel is treated for fluorography with Amplify and exposed during 3 days onto a photosensitive film. The fluorography is analysed using a Camag thin layer chromatography Scanner II densitometer.

Cell Research:[3]
  • Cell lines: ACHN, Caki-1, 786-O, and MCF-7 cells
  • Concentrations: ~ 5 mM
  • Incubation Time: 48 h
  • Method: 3.0×103 cells per well are seeded in a 96-well plate. After 24 h incubation, an optimum concentration gradient of elacridar is added to each well. After culturing for 48 h, cell viability is assessed using the proliferation reagent, MTT. Control cells are treated with the vehicle only, 0.1% DMSO. After this final incubation, the medium is aspirated and precipitated formazan crystals are dissolved in DMSO (100 μL/well). The absorbance of each well is measured at 540 nm, and a reference wavelength of 650 nm is read with a multiskan JX microplate reader. Cell viability is calculated as percentage of the control value.
Animal Research:[1]
  • Animal Models: Male wild-type, Abcb1a/1b-/-34, Abcg2 -/-32 and Abcb1a/1b;Abcg2
  • Dosages: 100 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

1mg/mL

Chemical Information

Molecular Weight 563.64
Formula

C34H33N3O5

CAS No. 143664-11-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=CC2=C1NC3=C(C2=O)C=CC=C3C(=O)NC4=CC=C(C=C4)CCN5CCC6=CC(=C(C=C6C5)OC)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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