Tariquidar (XR9576)

For research use only.

Catalog No.S8028

31 publications

Tariquidar (XR9576) Chemical Structure

CAS No. 206873-63-4

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.

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Selleck's Tariquidar (XR9576) has been cited by 31 publications

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Choose Selective P-gp Inhibitors

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 Mof1SpVv[3Srb36gZZN{[Xl? M3\XPFExODBibl2= M3jzWFczKGi{cx?= MoHDVI91\W62aXH0bY9vKG:oII\pcoNzcXO2aX7lMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2IuOy1zIHPlcIx{KGG|c3Xzd4VlKGG|II\pcoNzcXO2aX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSByLke4JEswNSByLkK3JI5OMSxiSVO1NF0xNjByMESx{txO Mo\kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
KBV1 MnfuSpVv[3Srb36gZZN{[Xl? NXK4fJdPOTByMDDuUS=> NUSwfWp1PzJiaILz MlPuTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hU0KYMTDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZidnnuZ5Jqe3SrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[nlibXXhd5VzcW6pII\pcoNzcXO2aX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB{N{euOlghMy9vIEW2MlYyKG6PKTygTWM2OD1yLkCwNFY3|ryP M1L3VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
HEK293 M{n4ZWZ2dmO2aX;uJIF{e2G7 MWixNFAxKG6P MlvCO|IhcHK| MYPQc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOg[I95d3K3YnnjbY4hUUN3MDDheEAyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG|c3H5JEhTfmJiPTC1MlI5KCtxLTCwMlc1KG6PKTygTWM2OD1yLkCwOFk2|ryP NUnoRYtxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
OVCAR8 M3r4OGZ2dmO2aX;uJIF{e2G7 Ml;kNVAxOCCwTR?= NFf6bZM4OiCqcoO= M3;ncHBwfGWwdHnheIlwdiCxZjD2bY5kemm|dHnu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUODDj[YxteyCjc4Pld5Nm\CCjczD2bY5kemm|dHnu[UBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iOD61N{AsNy1iMT65OUBvVSluIFnDOVA:OC5yMEWxPO69VQ>? NXvxR4RvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
KB-3-1 NH2wXmZHfW6ldHnvckBie3OjeR?= NXXlTHFWOTByMDDuUS=> MknBVI91\W62aXH0bY9vKG:oIHPvcINpcWOrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRk0{NTFiY3XscJMh[XO|ZYPz[YQh[XNiY3;sZ4hq[2mwZTDJR|UxKGG2IEGwNFAhdk1iYomgUXRVKGG|c3H5JEhTfmJiPTC4MlgyKCtxLTCzMlgxKG6PKTygTWM2OD1yLkCwPFQy|ryP MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzVyNE[2PUc,Ojd3MES2Olk9N2F-
KBV1 MYjGeY5kfGmxbjDhd5NigQ>? MXSxNFAxKG6P NEf3[oU4OiCqcoO= NY\Hc5ZWUW6qaXLpeIlwdiCxZjDoeY1idiCDQlPCNUBmgHC{ZYPz[YQhcW5iS1LWNUBk\WyuczDhd5Nme3OnZDDhd{Bxd3SnboTpZZRqd25ib3[gZ49t[2irY3nu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCkeTDt[YF{fXKrbnegZ49t[2irY3nu[UBKSzVyIHH0JFExODBibl2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTCoVpZjKD1iNEi3MlU4KCtxLTCzNE42PCCwTTmsJGlEPTB;MD6wNFkxPc7:TR?= NYLaT|NtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
MDCK NGe3TndHfW6ldHnvckBie3OjeR?= M2fPb|MxKG2rboO= M1POU2FkfGm4aYT5JIF1KEKFUmCgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hVUSFSzDj[YxteyC3c3nu[{BzcG:mYX3pcoUhOTJ|IHHzJJN2[nO2cnH0[UBqdmO3YnH0[YQh\m:{IEOwJI1qdnNicILpc5IhfG9ic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBGSzVyPUCuNFHPxE1? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5NEi3Nkc,OjN|N{S4O|I9N2F-
NCI-ADR-RES NGH4[ZNHfW6ldHnvckBie3OjeR?= MV[xNFAxKG6P M1qxbFczKGi{cx?= MkX3TY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hVkOLLVHEVk1TTVNiY3XscJMh[XO|ZYPz[YQh[XNicH;0[Y51cWG2aX;uJI9nKH[rbnPybZN1cW6nLXnu[JVk\WRiY4n0c5RwgGmlaYT5JIJ6KG2nYYP1dolv\yC4aX7jdol{fGmwZTDJR|UxKGG2IEGwNFAhdk1iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSBqUo\iJF0hOzdzND64NEAsNy1iM{izMlU5KG6PKTygTWM2OD1yLkCxPFUy|ryP NVHpUGY3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
OVCAR8 M3TlfGZ2dmO2aX;uJIF{e2G7 NVfYeoNGOTByMDDuUS=> NX\SXYxJPzJiaILz NInFO4NRd3SnboTpZZRqd25ib3[gZ49t[2irY3nu[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUODDj[YxteyCjc4Pld5Nm\CCjczDjc4xkcGmlaX7lJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSB{Nz6yOkAsNy1iOT65OkBvVSluIFnDOVA:OC5yMkO3N:69VQ>? M2i2clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
HEK293 MkPhSpVv[3Srb36gZZN{[Xl? MVixNFAxKG6P M3HTT|czKGi{cx?= MkeyTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMheG:2ZX70bYF1cW:wIH;mJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHL5JI1m[XO3cnnu[{Bld3ixcoXibYNqdiCLQ{WwJIF1KDFyMECgcm0h[W[2ZYKgO|IhcHK|IHL5JGNEUzhiYYPzZZkhMFK4YjC9JFUxPC54NTCrM{0hPDRwOUSgcm0qNCCLQ{WwQVAvODJ2N{hOwG0> NGXM[GE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WwOFY3QSd-Mke1NFQ3Pjl:L3G+
NCI-ADR-RES MX\GeY5kfGmxbjDhd5NigQ>? MnXENVAxOCCwTR?= NHLLS3I4OiCqcoO= MnOxTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMTDlfJBz\XO|ZXSgbY4hVkOLLVHEVk1TTVNiY3XscJMh[XO|ZYPz[YQh[XNicH;0[Y51cWG2aX;uJI9nKGOxbHPobYNqdmVvaX7keYNm\CCleYTveI95cWOrdImgZpkhdWWjc4XybY5oKGOxbHPobYNqdmViSVO1NEBifCBzMECwJI5OKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZkhMFK4YjC9JFE3ODdwNUCgL{8uKDR7Nz60NkBvVSluIFnDOVA:OC5yMkS5O:69VQ>? M2fzZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUC0OlY6Lz5{N{WwOFY3QTxxYU6=
CCRF-CEM/VCR1000 NYPUcGhiTnWwY4Tpc44h[XO|YYm= MWWyOFAhe2Wlcx?= MXLJcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMY1m\GmjdHXkJIRifW6xcoXibYNqdiCnZn\seZgh\nKxbTDoeY1idiCFQ2LGMWNGVS:YQ2KxNFAxKGOnbHzzJIFnfGW{IEK0NEB{\WO|IHL5JGZCS1NiZnzve{BkgXSxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVAvODN|MUJOwG0> NW[xTpFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0OVI1OTJpPkKyOFUzPDF{PD;hQi=>
MDCK MUfGeY5kfGmxbjDhd5NigQ>? NF3C[FA{OCCvaX7z Mo\4RYN1cX[rdImgZZQhVUSUMTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBOTEONIHPlcIx{KHW|aX7nJINidGOnaX6gRW0h[XNic4Xid5Rz[XSnIHnuZ5Vj[XSnZDDmc5IhOzBibXnud{BxemmxcjD0c{B{fWK|dILheIUh[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgN|AhdWmwczDifUBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFXDOVA:OC5yNEVOwG0> MkjDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{S4O|IoRjJ|M{e0PFczRC:jPh?=
MDCK NIrQRmhHfW6ldHnvckBie3OjeR?= M3W4Z|MxKG2rboO= NGjOVpNKdmirYnn0bY9vKG:oIGCt[4x6[2:ycn;0[YlvKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIF3ER2sh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHPhcINmcW5vQV2geJJidnOyb4L0JIFnfGW{IEOwJI1qdnNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBGSzVyPUCuNFQ1|ryP MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZyN{m5PUc,OjR4MEe5PVk9N2F-
EMT6/AR1.0 MmfOSpVv[3Srb36gZZN{[Xl? MUKxJIhz Ml3wTY5pcWKrdHnvckBw\iCvb4Xz[UBR\3BiaX6gSW1VPi:DUkGuNEBk\WyuczDh[pRmeiBzIHjyJIJ6KGSjdX7vdpVjcWOrbjDhZ4N2dXWuYYTpc44h[XO|YYmsJGlEPTB;MD6wOlTPxE1? MmHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyOEOwN|QoRjF6MEizNFM1RC:jPh?=
EMT6/AR1.0 NXPmfIVkTnWwY4Tpc44h[XO|YYm= M2Pk[lEhcHJ? NU\tO5NlUW6qaXLpeIlwdiCxZjDtc5V{\SCSZ4CgbY4hTU2WNj;BVlEvOCClZXzsd{Bi\nSncjCxJIhzKGK7IHTheY5wenWkaXPpckBi[2O3bYXsZZRqd25iYYPzZZktKEmFNUC9NE4xPjR3N988US=> NYPqeG5ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwPFMxOzRpPkG4NFg{ODN2PD;hQi=>
CEM/VLB500 MlS4SpVv[3Srb36gZZN{[Xl? NHPqUXY{KGSjeYO= M1viNXJmfmW{c3HsJI9nKFBvZ4CtcYVlcWG2ZXSgcZVtfGmmcoXnJJJme2m|dHHuZ4UhfG9idnnuZoxie3SrbnWgbY4hcHWvYX6gR2VON1[OQkWwNEBk\WyuczDh[pRmeiB|IHThfZMh[nlicnXzZZp2emmwIHHzd4F6NCCHQ{WwQVAvODZ6zszN NU\yPWhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezPVk6QTBpPkG3N|k6QTlyPD;hQi=>
KBV1 M3Xnc2Z2dmO2aX;uJIF{e2G7 NHf5fm0yODByIH7N NIfyXZM4OiCqcoO= MXnJcohq[mm2aX;uJI9nKGi3bXHuJGFDS0JzIHX4dJJme3OnZDDpckBMSlZzIHPlcIx{KGG|c3Xzd4VlKGG|IIDveIVvfGmjdHnvckBw\iCmb4jvdpVjcWOrbj3pcoR2[2WmIHP5eI91d3irY3n0fUBjgSCvZXHzeZJqdmdiZH;4c5J2[mmlaX6gTWM2OCCjdDCxNFAxKG6PIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XliKGL2ZkA:KDVwMEegL{8uKDBwMUmgeW0qNCCLQ{WwQVAvODgQvF2= NY\FOnl7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1NFQ3PjlpPkK3OVA1PjZ7PD;hQi=>
A2780 NFG1TWVHfW6ldHnvckBie3OjeR?= NXe4bos6UW6qaXLpeIlwdiCxZjDQMYdxKGmwIHj1cYFvKGGmcnnhcZlkcW5vcnXzbZN1[W62IFGyO|gxKGOnbHzzJIJ6KEixZXPod5QhOzN|NEKgZZN{[XluIFnDOVA:OC5yN{K0OO69VQ>? M4fQdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6Nke4OFk2Lz5zOE[3PFQ6PTxxYU6=
A2780/ADR M3vFU2Z2dmO2aX;uJIF{e2G7 MnHVTY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpck1u\WSrYYTl[EBufWy2aXTyeYchemW|aYP0ZY5k\SCrbjDh[JJq[W27Y3nuMZJme2m|dHHueEBpfW2jbjDBNlc5OC:DRGKgZ4VtdHNiYomgZ4Ft[2WrbjDBUUBie3OjeTygTWM2OD1yLkC3PO69VQ>? NUHEfIJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOVA5OzRpPkG5NlUxQDN2PD;hQi=>
A2780adr MYjGeY5kfGmxbjDhd5NigQ>? NHjvN2hKdmirYnn0bY9vKG:oIGCt[5Ah\XiycnXzd4VlKGmwIFGyO|gx[WS{IHPlcIx{KGK7IHPhcINmcW5iQV2gZYNkfW23bHH0bY9vKGG|c3H5MEBKSzVyPUCuNFjPxE1? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN3NEiwNEc,OjF|NUS4NFA9N2F-
OVCAR8 NHXPXI1HfW6ldHnvckBie3OjeR?= NVvWVnlrOTByMDDuUS=> NYK1Onc4PzJiaILz Mkn6VI91\W62aXH0bY9vKG:oIHTvfI9zfWKrY3nuMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJ6IHPlcIx{KGG|c3Xzd4VlKGG|IHTvfI9zfWKrY3nuJGlEPTBiYYSgNVAxOCCwTTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7IDjSeoIhRSByLkGyJEswNSByLkCzJJVOMSxiSVO1NF0xNjB6zszN MkLrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MES2OlkoRjJ5NUC0OlY6RC:jPh?=
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K562/A02 M{\tcmN6fG:2b4jpZ4l1gSCjc4PhfS=> MnLqOFghcHK| NVu0R|Y2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4Mj;BNFIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{Nz6xPe69VQ>? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ2NUizNUc,Ojh4NEW4N|E9N2F-
K562 M{nBWmN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3ROFghcHK| NHW4e5VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTNzLkW2{txO MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ|MUe4Okc,Ojl4M{G3PFY9N2F-
K562 NFjzeWFEgXSxdH;4bYNqfHliYYPzZZk> NUe4WlBQPDhiaILz NGjiXZFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9N|EvPTcQvF2= NX;ZRppDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OFU5OzFpPkK4OlQ2QDNzPD;hQi=>
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NB1643 MX;xTHRUKGG|c3H5 NIToNnNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz NF7JVIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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HepG2 NXPxfWJqTnWwY4Tpc44h[XO|YYm= M3PvflExKHWP MkjNPVAhdWmwcx?= MkLsTY5pcWKrdHnvckBw\iCSLXfwJI1m\GmjdHXkJIVn\my3eDDpckBi\HKrYX35Z4lvNXKnc3nzeIFvfCCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDpcpRz[WOnbHz1cIFzKHKqb3ThcYlv\S1zMkOgZYNkfW23bHH0bY9vKGG2IEGwJJVOKGmwY4XiZZRm\CCrbjDkZZJsKGOxbnTpeIlwdiCob4KgPVAhdWmwczDifUBndG:5IHP5eI9u\XS{eTDy[YxifGm4ZTD0c{Bkd262cn;s MmrCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MkiwNlkoRjJ5M{K4NFI6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Immunofluorescence
MRP7 ; 

PubMed: 23393594     


HEK/MRP7 cells were treated with 0.3 µM tariquidar for different periods of time. The subcellular localization of MRP7 was analyzed by immunofluorescence. MRP7 staining is shown in green. DAPI (blue) counterstains the nuclei.

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

Kinase Assay:

[1]

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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]

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  • 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.


    (Only for Reference)
Animal Research:

[3]

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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 646.73
Formula

C38H38N4O6

CAS No. 206873-63-4
Storage powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

P-gp Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID