Tariquidar (XR9576)

Catalog No.S8028

For research use only.

Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3.

Tariquidar (XR9576) Chemical Structure

CAS No. 206873-63-4

Selleck's Tariquidar (XR9576) has been cited by 34 publications

Purity & Quality Control

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Biological Activity

Description Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3.
Targets
P-gp [1]
(CHrB30 cells)
5.1 nM(Kd)
In vitro

Tariquidar displays high-affinity binding to P-gp with Bmax of 275 pmol/mg. Tariquidar shows non-competitive interaction with the P-gp substrates vinblastine and paclitaxel. Tariquidar increases the steady-state accumulation of these cytotoxics in CHrB30 cells to levels observed in non-P-gp-expressing AuxB1 cells with EC50 of 487 nM. Tariquidar is able to inhibit the vanadate-sensitive ATPase activity of P-gp by 60-70%, with potent IC50 values of 43 nM. [1] Tariquidar may inhibit other resistance mechanisms at higher concentrations. 1 μM Tariquidar abrogates ABCG2 (BCRP)-mediated resistance to camptothecins in vitro. [2] Tariquidar potentiates the cyto-toxicity of several drugs including doxorubicin, paclitaxel, etoposide, and vincristine; complete reversal of resistance is achieved in the presence of 25- 80 nM Tariquidar. In MC26, a murine colon carcinoma cell line with intrinsic chemoresistance, the doxorubicin IC50 is fivefold lower in the presence of 0.1 μM Tariquidar (36 vs 7 nM). In murine mammary carcinoma, human small-cell lung carcinoma and human ovarian carcinoma cell lines with acquired chemotherapeutic resistance (EMT6/AR1.0, H69/LX4 and 2780 AD), the in vitro doxorubicin IC50 is 22-150-fold lower in the presence of 0.1 μM Tariquidar. P-gp inhibition persists for 23 h after removal of Tariquidar from the culture system. [3] Tariquidar restored the cyto-toxicity of doxorubicin and vinblastine in the National Cancer Institute (NCI)/ADRRES multicellular tumor spheroid model derived from the MCF7WT breast cancer cell line. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-3-1 MYjGeY5kfGmxbjDhd5NigQ>? MoSwNVAxOCCwTR?= NVn6VlFFPzJiaILz NFvaOolRd3SnboTpZZRqd25ib3[geolv[3Krc4TpcoUucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSi1|LUGgZ4VtdHNiYYPz[ZN{\WRiYYOgeolv[3Krc4TpcoUhUUN3MDDheEAyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmgLHJ3[iB;IECuO|ghMy9vIECuNlchdk1rLDDJR|UxRTBwMECwOFHPxE1? M4XqfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
KBV1 MVfGeY5kfGmxbjDhd5NigQ>? NIDIfW0yODByIH7N NGSxbGo4OiCqcoO= NUi3c|F5UW6qaXLpeIlwdiCxZjDoeY1idiCDQlPCNUBmgHC{ZYPz[YQhcW5iS1LWNUBk\WyuczDhd5Nme3OnZDDhd{Bxd3SnboTpZZRqd25ib3[geolv[3Krc4TpcoUucW6mdXPl[EBkgXSxdH;4bYNqfHliYomgcYVie3W{aX7nJJZqdmO{aYP0bY5mKEmFNUCgZZQhOTByMDDuUUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5JEhTfmJiPTCyO|cvPjhiKz:tJFU3NjZzIH7NLUwhUUN3ME2wMlAxODZ4zszN NI[zZmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WwOFY3QSd-Mke1NFQ3Pjl:L3G+
HEK293 MYfGeY5kfGmxbjDhd5NigQ>? M1j2fVExODBibl2= NY[1bmNKPzJiaILz MYDQc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOg[I95d3K3YnnjbY4hUUN3MDDheEAyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG|c3H5JEhTfmJiPTC1MlI5KCtxLTCwMlc1KG6PKTygTWM2OD1yLkCwOFk2|ryP MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
OVCAR8 M1TodWZ2dmO2aX;uJIF{e2G7 NH:4bXQyODByIH7N M3S3WVczKGi{cx?= M2TmU3BwfGWwdHnheIlwdiCxZjD2bY5kemm|dHnu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUODDj[YxteyCjc4Pld5Nm\CCjczD2bY5kemm|dHnu[UBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iOD61N{AsNy1iMT65OUBvVSluIFnDOVA:OC5yMEWxPO69VQ>? NVnWS5JxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
KB-3-1 MUjGeY5kfGmxbjDhd5NigQ>? M37aTlExODBibl2= M2\Kd3BwfGWwdHnheIlwdiCxZjDjc4xkcGmlaX7lMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2IuOy1zIHPlcIx{KGG|c3Xzd4VlKGG|IHPvcINpcWOrbnWgTWM2OCCjdDCxNFAxKG6PIHL5JG1VXCCjc4PhfUApWn[kIE2gPE45OSBtLz2gN{45OCCwTTmsJGlEPTB;MD6wNFg1Oc7:TR?= M{PoNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
KBV1 MlzUSpVv[3Srb36gZZN{[Xl? NXzY[GR3OTByMDDuUS=> M1zHb|czKGi{cx?= MnO5TY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hU0KYMTDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZiY3;sZ4hq[2mwZT3pcoR2[2WmIHP5eI91d3irY3n0fUBjgSCvZXHzeZJqdmdiY3;sZ4hq[2mwZTDJR|UxKGG2IEGwNFAhdk1iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSBqUo\iJF0hPDh5LkW3JEswNSB|MD61OEBvVSluIFnDOVA:OC5yMEmwOe69VQ>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
MDCK NHnzbGFHfW6ldHnvckBie3OjeR?= NXq2cpJbOzBibXnudy=> Mn\0RYN1cX[rdImgZZQhSkOUUDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBOTEONIHPlcIx{KHW|aX7nJJJpd2SjbXnu[UAyOjNiYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiM{CgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGVEPTB;MD6wNe69VQ>? NVHpUpg3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|Q5PzJpPkKzN|c1QDd{PD;hQi=>
NCI-ADR-RES NYPzbJZxTnWwY4Tpc44h[XO|YYm= MkT2NVAxOCCwTR?= Mk\KO|IhcHK| NHPFbG5KdmirYnn0bY9vKG:oIHj1cYFvKEGEQ1KxJIV5eHKnc4Pl[EBqdiCQQ1mtRWRTNVKHUzDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZidnnuZ5Jqe3SrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[nlibXXhd5VzcW6pII\pcoNzcXO2aX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB|N{G0MlgxKCtxLTCzPFMvPThibl2pMEBKSzVyPUCuNFE5PTIQvF2= M3Hz[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
OVCAR8 MnfqSpVv[3Srb36gZZN{[Xl? MknxNVAxOCCwTR?= M3z2[VczKGi{cx?= MVPQc5RmdnSrYYTpc44hd2ZiY3;sZ4hq[2mwZT3pcoR2[2WmIHP5eI91d3irY3n0fUBi\2GrboP0JIh2dWGwIF;WR2FTQCClZXzsd{Bie3Onc4Pl[EBieyClb3zjbIlkcW6nIFnDOVAh[XRiMUCwNEBvVSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6KCiUdnKgQUAzPy5{NjCrM{0hQS57NjDuUUktKEmFNUC9NE4xOjN5M988US=> Mn63QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
HEK293 MXPGeY5kfGmxbjDhd5NigQ>? NHfLO2IyODByIH7N M13RTlczKGi{cx?= Mo\XTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMheG:2ZX70bYF1cW:wIH;mJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHL5JI1m[XO3cnnu[{Bld3ixcoXibYNqdiCLQ{WwJIF1KDFyMECgcm0h[W[2ZYKgO|IhcHK|IHL5JGNEUzhiYYPzZZkhMFK4YjC9JFUxPC54NTCrM{0hPDRwOUSgcm0qNCCLQ{WwQVAvODJ2N{hOwG0> M2e3NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
NCI-ADR-RES NELZT5hHfW6ldHnvckBie3OjeR?= NXTrd|c2OTByMDDuUS=> NX75fWl1PzJiaILz M1vtRmlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFQkGg[ZhxemW|c3XkJIlvKE6FST3BSHIuWkWVIHPlcIx{KGG|c3Xzd4VlKGG|IIDveIVvfGmjdHnvckBw\iClb3zjbIlkcW6nLXnu[JVk\WRiY4n0c5RwgGmlaYT5JIJ6KG2nYYP1dolv\yClb3zjbIlkcW6nIFnDOVAh[XRiMUCwNEBvVSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6KCiUdnKgQUAyPjB5LkWwJEswNSB2OUeuOFIhdk1rLDDJR|UxRTBwMEK0PVfPxE1? M3TpflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
CCRF-CEM/VCR1000 M3e3SGZ2dmO2aX;uJIF{e2G7 M{P5SVI1OCC|ZXPz M3\oOGlvcGmkaYTpc44hd2ZiUD3ncJlkd3C{b4TlbY4udWWmaXH0[YQh\GG3bn;yeYJq[2mwIHXm[ox2gCCocn;tJIh2dWGwIFPDVmYuS0WPL2\DVlExODBiY3XscJMh[W[2ZYKgNlQxKHOnY4OgZpkhTkGFUzDmcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OC5yM{OxNe69VQ>? NWnFcldKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0OVI1OTJpPkKyOFUzPDF{PD;hQi=>
MDCK MonPSpVv[3Srb36gZZN{[Xl? NH7XTnA{OCCvaX7z M4rtRmFkfGm4aYT5JIF1KE2GUkGgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hVUSFSzDj[YxteyC3c3nu[{Bk[WylZXnuJGFOKGG|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDNyIH3pcpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDFR|UxRTBwMES0{txO M2nXWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{e0PFczLz5{M{O3OFg4OjxxYU6=
MDCK MX7GeY5kfGmxbjDhd5NigQ>? MYKzNEBucW6| MkLLTY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpckApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCPRFPLJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClYXzj[YlvNUGPIITyZY5{eG:{dDDh[pRmeiB|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygSWM2OD1yLkC0OO69VQ>? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZyN{m5PUc,OjR4MEe5PVk9N2F-
EMT6/AR1.0 NGm0SFVHfW6ldHnvckBie3OjeR?= M4TSZVEhcHJ? MX3Jcohq[mm2aX;uJI9nKG2xdYPlJHBoeCCrbjDFUXQ3N0GUMT6wJINmdGy|IHHmeIVzKDFiaIKgZpkh\GG3bn;yeYJq[2mwIHHjZ5VufWyjdHnvckBie3OjeTygTWM2OD1yLkC2OO69VQ>? NGDnPII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC4N|A{PCd-MUiwPFMxOzR:L3G+
EMT6/AR1.0 NFjqNmJHfW6ldHnvckBie3OjeR?= MUixJIhz Ml;1TY5pcWKrdHnvckBw\iCvb4Xz[UBR\3BiaX6gSW1VPi:DUkGuNEBk\WyuczDh[pRmeiBzIHjyJIJ6KGSjdX7vdpVjcWOrbjDhZ4N2dXWuYYTpc44h[XO|YYmsJGlEPTB;MD6wOlQ2P87:TR?= Mo\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyOEOwN|QoRjF6MEizNFM1RC:jPh?=
CEM/VLB500 MXzGeY5kfGmxbjDhd5NigQ>? MUmzJIRigXN? NI\jRWhT\X[ncoPhcEBw\iCSLXfwMY1m\GmjdHXkJI12dHSrZIL1[{Bz\XOrc4ThcoNmKHSxII\pcoJt[XO2aX7lJIlvKGi3bXHuJGNGVS:YTFK1NFAh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IILld4F7fXKrbjDhd5NigSxiRVO1NF0xNjB4ON88US=> M2OwclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{m5PVkxLz5zN{O5PVk6ODxxYU6=
KBV1 MlflSpVv[3Srb36gZZN{[Xl? MoLENVAxOCCwTR?= NVu3eFY6PzJiaILz M1fwVmlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFQkGg[ZhxemW|c3XkJIlvKEuEVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgdI91\W62aXH0bY9vKG:oIHTvfI9zfWKrY3nuMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGK7IH3lZZN2emmwZzDkc5hwenWkaXPpckBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iNT6wO{AsNy1iMD6xPUB2VSluIFnDOVA:OC5yN988US=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
A2780 MoH6SpVv[3Srb36gZZN{[Xl? MkjjTY5pcWKrdHnvckBw\iCSLXfwJIlvKGi3bXHuJIFlemmjbYnjbY4uemW|aYP0ZY51KEF{N{iwJINmdGy|IHL5JGhw\WOqc4SgN|M{PDJiYYPzZZktKEmFNUC9NE4xPzJ2NN88US=> NFHTe249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[3PFQ6PSd-MUi2O|g1QTV:L3G+
A2780/ADR M3zuZmZ2dmO2aX;uJIF{e2G7 MULJcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMY1m\GmjdHXkJI12dHSrZIL1[{Bz\XOrc4ThcoNmKGmwIHHkdolidXmlaX6tdoV{cXO2YX70JIh2dWGwIFGyO|gxN0GGUjDj[YxteyCkeTDjZYxk\WmwIFHNJIF{e2G7LDDJR|UxRTBwMEe4{txO NIDTXWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK1NFg{PCd-MUmyOVA5OzR:L3G+
A2780adr NWLWfnJlTnWwY4Tpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKFBvZ4Cg[ZhxemW|c3XkJIlvKEF{N{iwZYRzKGOnbHzzJIJ6KGOjbHPlbY4hSU1iYXPjeY12dGG2aX;uJIF{e2G7LDDJR|UxRTBwMElOwG0> MmLtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NUS4NFAoRjJzM{W0PFAxRC:jPh?=
OVCAR8 NVnrUZZLTnWwY4Tpc44h[XO|YYm= M2LqNlExODBibl2= M{ezd|czKGi{cx?= MWfQc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[XO|ZYPz[YQh[XNiZH;4c5J2[mmlaX6gTWM2OCCjdDCxNFAxKG6PIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XliKGL2ZkA:KDBwMUKgL{8uKDBwMEOgeW0qNCCLQ{WwQVAvODkQvF2= NXnRUXhwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
KB-3-1 NGj6NoFHfW6ldHnvckBie3OjeR?= NW\lfZB7OTByMDDuUS=> NWr4eVd1PzJiaILz NE\vPXdRd3SnboTpZZRqd25ib3[g[I95d3K3YnnjbY4ucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSi1|LUGgZ4VtdHNiYYPz[ZN{\WRiYYOg[I95d3K3YnnjbY4hUUN3MDDheEAyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmgLHJ3[iB;IECuNVUhMy9vIECuNFQhfU1rLDDJR|UxRTBwMUJOwG0> NVLjRW96RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
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Assay
Methods Test Index PMID
Immunofluorescence MRP7 23393594
In vivo Tariquidar (2- 8 mg/kg p.o.) is found to significantly potentiate the antitumor activity of doxorubicin (5 mg/kg, i.v.) against MC26 murine colon carcinoma in vivo. In human carcinoma xenografts, coadministration of XR9576 (6 -12 mg/kg p.o.) fully restored the antitumor activity of paclitaxel, etoposide, and vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. [3]

Protocol (from reference)

Kinase Assay:

[1]

  • Steady-state drug accumulation assay:

    AuxB1 and CHrB30 cells are grown to confluency in 12-well (24 mm) tissue culture dishes and the steady-state accumulation of [3H]-vinblastine is measured. Accumulation is initiated by the addition of 0.1 μ Ci [3H]-vinblastine and unlabelled vinblastine to a final concentration of 100 nM . The accumulation of [3H]-paclitaxel is measured using 0.1 μ Ci [3H]-paclitaxel and unlabelled drug to a final concentration of 1 μM . Cells are incubated in a reaction volume of 1 mL for 60 min at 37 ℃ under 5% CO2 in order to reach steady-state. The effect of the modulators XR9576 on [3H]-ligand accumulation is investigated in the concentration range 10-9 - 10-6 M. Modulators are added from a DMSO stock giving a final solvent concentration of 0.2 % (v/v). Following cell harvesting, accumulated drug is measured by liquid scintillation counting and normalized for cell protein content. Plots of amount accumulated as a function of modulator concentration are fitted with the general dose-response equation: Y={(a-b)/(1+(X/c)d)}+bWhere: Y=response; a=initial response; b=final response; c=EC50 concentration; d=slope value; X=drug concentration.

Cell Research:

[3]

  • Cell lines: Murine mammary carcinoma cell line MDR EMT6/AR1.0
  • Concentrations: ~100 nM Tariquidar
  • Incubation Time: 4 days
  • Method:

    Cells are seeded into 96-well plates at 800/well, in 100 μL of medium and incubated for 4 h at 37 ℃. Varying concentrations of modulator or solvent control (50 μL/well) are subsequently added and incubated for an additional 1 h before the addition of the cytotoxic drug. The cytotoxic drug (50 μL) is added to give a range of final concentrations in quadruplicate wells. After incubation for an additional 4 days, cell proliferation of adherent cells is assessed using the sulforhodamine B assay.

Animal Research:

[3]

  • Animal Models: Murine colon carcinoma xenografts MC26
  • Dosages: 8 mg/kg
  • Administration: Coadministration of Tariquidar (p.o.) with doxorubicin (5 mg/kg, i.v.)

Solubility (25°C)

In vitro

DMSO 52 mg/mL
(80.4 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 646.73
Formula

C38H38N4O6

CAS No. 206873-63-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)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

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01663545 Completed -- Epilepsies Partial National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC) July 31 2012 --
NCT01547754 Terminated -- HIV-Associated Cognitive Motor Complex National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC) January 9 2012 --
NCT01386476 Completed -- Drug Resistance National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC) June 15 2011 --
NCT00082368 Completed Drug: Tariquidar|Drug: Tc-94m Sestamibi Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 16 2004 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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Frequently Asked Questions

Question 1:
Can you please give me more specific and detailed information of how to dissolve and use this compound (S8028) for in vivo studies?

Answer:
Tariquidar in 30% Propylene glycol, 5% Tween 80, 65% D5W at 30mg/ml will be a suspension or emulsion. If you are going to administrate the compound by oral gavage, it is fine. We also have test some vehicles for Tariquidar for i.p injection, and it is soluble in 5% DMSO+45% PEG 300+ddH2O at 2mg/ml clearly. When preparing the solution, please dissolve the compound in DMSO clearly first, then add PEG. After they mixed well, then dilute with water.

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