Tariquidar (XR9576)

Name: Tariquidar (XR9576)
Brand: Selleck Chemicals
SKU: S8028
Rating: 5 (31 reviews)

For research use only.

Catalog No.S8028

31 publications

CAS No. 206873-63-4

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

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

Nat Commun, 2021, 12(1):617

PubMed: 33504784 ( click the link to review the publication )

Front Oncol, 2021, 11:620907

PubMed: 33738259 ( click the link to review the publication )

Mol Syst Biol, 2020, 16(3):e9195

PubMed: 32187448 ( click the link to review the publication )

Cancers (Basel), 2020, 30;12(5) pii: E1123

PubMed: 32365878 ( click the link to review the publication )

Neurosurgery, 2020, 1;86(5):742-751

PubMed: 31225627 ( click the link to review the publication )

Sci Rep, 2020, 26;10(1):8671

PubMed: 32457334 ( click the link to review the publication )

Blood Adv, 2020, 4(20):5062-5077

PubMed: 33080008 ( click the link to review the publication )

J Clin Invest, 2019, 129(10):4377-4392

PubMed: 31498151 ( click the link to review the publication )

Cancer Res, 2019, 10.1158/0008-5472.CAN-18-1888

PubMed: 30630822 ( click the link to review the publication )

J Control Release, 2019, 317:67-77

PubMed: 31756395 ( click the link to review the publication )

Breast Cancer Res, 2019, 21(1):7

PubMed: 30654824 ( click the link to review the publication )

Mol Cancer Res, 2019, 17(11):2196-2207

PubMed: 31444231 ( click the link to review the publication )

Front Physiol, 2019, 10:616

PubMed: 31178753 ( click the link to review the publication )

Cancer Biol Ther, 2019, 10.1080/15384047.2019.1683324

PubMed: 31709896 ( click the link to review the publication )

Molecules, 2019, 24(3)

PubMed: 30717494 ( click the link to review the publication )

Oncogene, 2018, 37(2):208-217

PubMed: 28925391 ( click the link to review the publication )

Cell Chem Biol, 2018, 25(2):135-142

PubMed: 29276047 ( click the link to review the publication )

Sci Rep, 2018, 8(1):11429

PubMed: 30061701 ( click the link to review the publication )

Acta Pharmacol Sin, 2018, 39(6):1048-1063

PubMed: 29620050 ( click the link to review the publication )

Ann Biomed Eng, 2018, 46(6):899-911

PubMed: 29484528 ( click the link to review the publication )

Bioinformation, 2018, 587-593

PubMed: 31223218 ( click the link to review the publication )

Nat Chem Biol, 2017, 13(2):168-173

PubMed: 27918558 ( click the link to review the publication )

Toxicol In Vitro, 2017, 44:241-247

PubMed: 28746893 ( click the link to review the publication )

Leuk Lymphoma, 2017, 58(12):2916-2925

PubMed: 28509582 ( click the link to review the publication )
Int J Ophthalmol, 2017, 10(7):1055-1063

PubMed: 28730106 ( click the link to review the publication )

Oncotarget, 2017, 8(5):7678-7690

PubMed: 28032595 ( click the link to review the publication )

J Med Chem, 2016, 59(13):6353-69

PubMed: 27328029 ( click the link to review the publication )

Biochem Pharmacol, 2016, 101:40-53

PubMed: 26686578 ( click the link to review the publication )

Am J Transl Res, 2015, 7(6):1009-20

PubMed: 26279746 ( click the link to review the publication )

Vet Parasitol, 2015, 211(1-2):80-8

PubMed: 25986327 ( click the link to review the publication )

Mol Med Rep, 2015, 12(6):8093-100

PubMed: 26496964 ( click the link to review the publication )

Purity & Quality Control

Choose Selective P-gp Inhibitors

Biological Activity

Description

Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with K_d 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 B_max 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 CH^rB30 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)/ADR^RES multicellular tumor spheroid model derived from the MCF7^WT breast cancer cell line. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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=>
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HCT116	MoLLR5l1d3SxeHnjbZR6KGG\|c3H5		MXu0PEBpenN?	MmLBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG\|c3Xzd4VlKGG\|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVIvPc7:TR?=	NF2yVXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG5O\|E3OCd-Mk[xPVcyPjB:L3G+
MCF7/ADR	M2HkSWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MoTjOFghcHK\|	MVLJcpRzcW6\|aXOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPy:DRGKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yOy5zzszN	NELrUHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OyPFAzQSd-MkezNlgxOjl:L3G+
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K562/A02	MY\GeY5kfGmxbjDhd5NigQ>?		MUC0PEBpenN?	NETkZm1KdmirYnn0bY9vKG:oIFHCR2IyKGmwIHj1cYFvKEt3NkKvRVAzKGOnbHzzJIF{e2W\|c3XkJIF{KHCxdHXueIlifGmxbjDv[kBi\HKrYX35Z4lvNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHL5JI1m[XO3cnnu[{BCTFJiSVO1NEB1emWjdHXkJIZweiB2ODDodpMh\m:ubH;3[YQh[nliY3;tdI92dmRid3HzbI92fCCvZXHzeZJm\CCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6KCiUdnKgQUA2OS5\|NDCrM{0hPS5zIIXNLUwhUUN3ME2xOE4{Qc7:TR?=	NUTkOpN[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OFU5OzFpPkK4OlQ2QDNzPD;hQi=>
HLF	NX7vS5Y3S3m2b4TvfIlkcXS7IHHzd4F6		MWG0PEBpenN?	NHLaUnpEgXSxdH;4bYNqfHliYXfhbY5{fCCKTF[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yPi54Od88US=>	MkC0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd\|MkiwNlkoRjJ5M{K4NFI6RC:jPh?=
SW620	NIjkd3FEgXSxdH;4bYNqfHliYYPzZZk>		NW\LZ4dHPDhiaILz	MknyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3c3OjBiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2yOe69VQ>?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF7N{G2NEc,OjZzOUexOlA9N2F-
SW620/AD300	M1nVSGN6fG:2b4jpZ4l1gSCjc4PhfS=>		NH7nSFM1QCCqcoO=	M1TG[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyL1HEN\|AxKGOnbHzzJIF{e2W\|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;MkZOwG0>	MkeyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOUexOlAoRjJ4MUm3NVYxRC:jPh?=
CCD-18Co	M3[3NWN6fG:2b4jpZ4l1gSCjc4PhfS=>		NWnjNFVRPDhiaILz	MkX4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NFNTF6Q3:gZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0zPc7:TR?=	NWG2R5lURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPVcyPjBpPkK2NVk4OTZyPD;hQi=>
K562/A02	MUjDfZRwfG:6aXPpeJkh[XO\|YYm=		NEfib3o1QCCqcoO=	NW\RbpZES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4Mj;BNFIh[2WubIOgc5ZmemW6cILld5NqdmdiUD3ndEBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0zPy5zOd88US=>	Mn3KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4M{G3PFYoRjJ7NkOxO\|g3RC:jPh?=
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=>
HepG2	M2TiV2N6fG:2b4jpZ4l1gSCjc4PhfS=>		M3jtZVQ5KGi{cx?=	Mlu0R5l1d3SxeHnjbZR6KGGpYXnud5Qh[WS{aXHtfYNqdi2{ZYPpd5RidnRiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0{Py5{zszN	M1X5bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{K4NFI6Lz5{N{OyPFAzQTxxYU6=
KB-V1	M4LqN2Z2dmO2aX;uJIF{e2G7	NEH2cJgzODBibl2=		MoDWTY5pcWKrdHnvckBw\iCSLXfwJIlvKGi3bXHuJGtDNVZzIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnuZ5Jm[XOnIHnuJJJpd2SjbXnu[UAyOjNiYXPjeY12dGG2aX;uJIF1KDJyMDDuUS=>	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ3N{K3NUc,OjF4NUeyO\|E9N2F-
SK-N-MC	NWnwS5FMeUiWUzDhd5NigQ>?			Ml;HdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO=	M4XDR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH	Mn3ndWhVWyCjc4PhfS=>			NH[xc5FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=>	M4P3V\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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+
K562/DOX	NVzFU5h6TnWwY4Tpc44h[XO\|YYm=	NYjVPIFFOSC3TR?=	MlPuNVAhdWmwcx?=	MW\Jcohq[mm2aX;uJI9nKFBvZ4CgbY4hcHWvYX6gT\|U3Oi:GT2igZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hemixZHHtbY5mNTF{MzDl[oZtfXhiaX6gbJVu[W5iS{W2NkBk\WyuczDheEAyKHWPIHnuZ5Vj[XSnZDDmc5IhOTBibXnud{BpenNiYomg[oxwfyCleYTvcYV1enlicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3y=	MlrpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzMUOxNlgoRjJ6MUGzNVI5RC:jPh?=
A2780adr	NVjwTXJ6TnWwY4Tpc44h[XO\|YYm=	MlvjNVAhfU1?	MWGzNEBucW6\|	NYXublhmUW6qaXLpeIlwdiCxZjDBRmNDOSCrbjDoeY1idiCDMke4NIFleiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDhZ4N2dXWuYYTpc44hd2ZiY3HsZ4VqdiCDTTDheEAyOCC3TTDwdoVqdmO3YnH0[YQh\m:{IEOwJI1qdnNiZn;scI94\WRiYomgZ4Ft[2WrbjDBUUBi\GSrdHnvckBu\WG\|dYLl[EBmfmW{eTC2NEB{\WO\|IH\vdkA3OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSC{ZXzheIl3\SC2bzDjc451em:u	NX[xT5RjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OFczPzJpPkK5OVQ4Ojd{PD;hQi=>
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 PLoS One 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]	- Collapse Steady-state drug accumulation assay: AuxB1 and CH^rB30 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]	- Collapse 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]	- Collapse 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)

References

[4] Walker J, et al. Eur J Cancer, 2004, 40(4), 594-605.

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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 Download Tariquidar (XR9576) SDF

Molecular Weight	646.73
Formula	C₃₈H₃₈N₄O₆
CAS No.	206873-63-4
Storage	3 years-20°C powder 2 years-80°C 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

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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.

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

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.

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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Tariquidar (XR9576)