Tariquidar

Catalog No.S8028 Synonyms: XR9576

Tariquidar Chemical Structure

Molecular Weight(MW): 646.73

Tariquidar 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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In DMSO USD 220 In stock
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Cited by 20 Publications

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Biological Activity

Description Tariquidar 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
MDCK cells NHLNbZpHfW6ldHnvckBie3OjeR?= MUmzNEBucW6| NYjwc|RqSWO2aY\peJkh[XRiQlPSVEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCPRFPLJINmdGy|IIXzbY5oKHKqb3ThcYlv\SBzMkOgZZMhe3Wkc4TyZZRmKGmwY4XiZZRm\CCob4KgN|AhdWmwczDwdolweiC2bzDzeYJ{fHKjdHWgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiM{CgcYlveyCkeTDmcJVwem:vZYTybYMh[W6jbInzbZMtKEWFNUC9NE4xOSEQvF2= NFPvd44zOzN5NEi3Ni=>
EMT6/AR1.0 cells NVToZ4h6TnWwY4Tpc44h[XO|YYm= NWG2[ZVKOSCq NFL6dGpKdmirYnn0bY9vKG:oIH3veZNmKFCpcDDpckBGVVR4L1HSNU4xKGOnbHzzJIFnfGW{IEGgbJIh[nliZHH1co9zfWKrY3nuJIFk[3WvdXzheIlwdiCjc4PhfUwhUUN3ME2wMlA3PCEQvF2= M2Tl[lE5ODh|MEO0
human CEM/VLB500 cells NV3zfWNiTnWwY4Tpc44h[XO|YYm= MXuzJIRigXN? M2D1eXJmfmW{c3HsJI9nKFBvZ4CtcYVlcWG2ZXSgcZVtfGmmcoXnJJJme2m|dHHuZ4UhfG9idnnuZoxie3SrbnWgbY4hcHWvYX6gR2VON1[OQkWwNEBk\WyuczDh[pRmeiB|IHThfZMh[nlicnXzZZp2emmwIHHzd4F6NCCHQ{WwQVAvODZ6IN88US=> NIrRTYgyPzN7OUm5NC=>
A2780 cells NYHTVJhITnWwY4Tpc44h[XO|YYm= MWqzNEBucW6| NHLQUoZKdmirYnn0bY9vKG:oIHj1cYFvKFCpcDDpckBCOjd6MDDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KEixZXPod5QhOzN|NEKgZZN{[XluIFnDOVA:OC5zMkW4PUDPxE1? NIjVUHkyQDB6M{CzOC=>
human KBV1 cells NXXvVnc4TnWwY4Tpc44h[XO|YYm= NULCe4d2OTBibXnudy=> NVnScpdnUW6qaXLpeIlwdiCxZjDBRmNDOSCrbjDoeY1idiCNQm[xJINmdGy|IHHmeIVzKDFyIH3pcpMh[nliQ3HsZ4Vqdi2DTTDtbYNzd3CuYYTlJIF{e2G7LDDJR|UxRTBwMkKzJO69VQ>? NIroTVgzPDlyME[4Ny=>
human MCF7/Topo cells MVrGeY5kfGmxbjDhd5NigQ>? NHTWeVlKdmirYnn0bY9vKG:oIFHCR2czKGW6cILld5Nm\CCrbjDoeY1idiCPQ1[3M3RweG9iY3XscJMh[nliSH;lZ4h{fCCvaXPyc5Bt[XSnIHHzd4F6NCCLQ{WwQVAvPTJ4IN88US=> NIr2bYEzOTV5MEK4Ni=>
MCF7 MX cells MoL1SpVv[3Srb36gZZN{[Xl? NUPLdmJ7UW6qaXLpeIlwdiCxZjDCR3JRKGW6cILld5Nm\CCrbjDNR2Y4KE2[IHPlcIx{KGK7IFjv[YNpe3RiM{OzOFIhe3SjaX7pcoctKEmFNUC9NE43QCEQvF2= MV:xPVk{Ojl4MB?=
human HFE cells MXHDfZRwfG:6aXRCpIF{e2G7 MV[3NkBp Ml3lR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGZGKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6yPEDPxE1? NHS3SFEzPjF7N{G2NC=>
human HCT116 cells MmrlR5l1d3SxeHnjxsBie3OjeR?= MV20PEBp M{P5bGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEzNjVizszN M1KxOVI3OTl5MU[w
human SW620 cells MWrDfZRwfG:6aXRCpIF{e2G7 NUiyfG9JPDhiaB?= M13mc2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NlUh|ryP NYPmN2tTOjZzOUexOlA>
human SW620/AD300 cells NH;sfGxEgXSxdH;4bYPDqGG|c3H5 M4HhZ|Q5KGh? NGPiWo9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXzZ{MD;BSFMxOCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUK1JO69VQ>? NXTINolVOjZzOUexOlA>
human CCD-18Co cells NXm4NpFwS3m2b4TvfIlkyqCjc4PhfS=> M2SzU|Q5KGh? MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDR2QuOTiFbzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI2KM7:TR?= MmjRNlYyQTdzNkC=
human KB-V1 cells MY\GeY5kfGmxbjDhd5NigQ>? M3HaPVIxOCCwTR?= NULIcpE5UW6qaXLpeIlwdiCxZjDQMYdxKGmwIHj1cYFvKEuELW[xJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKHKqb3ThcYlv\SBzMkOgZYNkfW23bHH0bY9vKGG2IEKwNEBvVQ>? MWKyNVY2PzJ5MR?=

... 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
  • Formulation: 5% (w/v) D-( 1)-glucose (dextrose) solution
  • 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
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% Propylene glycol+5% Tween 80+65% D5W
For best results, use promptly after mixing.
30mg/mL

* 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 XR9576

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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.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID