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    Tariquidar (XR9576)
    Tariquidar (XR9576)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1295
    CAS #: 206873-63-4 Purity ≥98%

    Description: Tariquidar (formerly XR9576; D06008; XR-9576; D-06008) is a potent and selective noncompetitive inhibitor of P-glycoprotein  (P-gp) with potential antineoplastic activity. It inhibits P-gp with a Kd of 5.1 nM in CHrB30 cell line, it reverses drug resistance in MDR cell Lines. Tariquidaris is currently undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs. Inhibition of transmembrane transport may result in increased intracellular concentrations of an anticancer drug, thereby augmenting its cytotoxicity. 

    References: Br J Pharmacol. 1999 Sep;128(2):403-11; Cancer Res. 2001 Jan 15;61(2):749-58.

    Related CAS#: 625375-84-0 (dimesylate); 625375-83-9 (dimesylate hydrate); 206873-63-4 (free base)

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    Molecular Weight (MW)646.73
    FormulaC38H38N4O6
    CAS No.206873-63-4 (free base)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 52 mg/mL (80.4 mM)
    Water:<1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    SynonymsXR9576; D06008; XR 9576; D 06008; XR-9576; D-06008


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    In Vitro

    In vitro activity: 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 CHr<>/supB30 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. Tariquidar may inhibit other resistance mechanisms at higher concentrations. 1 μM Tariquidar abrogates ABCG2 (BCRP)-mediated resistance to camptothecins in vitro. 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. 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. 


    Kinase 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)}+b Where: Y=response; a=initial response; b=final response; c=EC50 concentration; d=slope value; X=drug concentration.


    Cell Assay: 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.

    In VivoTariquidar (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.
    Animal modelMurine colon carcinoma xenografts MC26
    Formulation & DosageDissolved in5% (w/v) D-( 1)-glucose (dextrose) solution; 8 mg/kg ; Coadministration of Tariquidar (p.o.) with doxorubicin (5 mg/kg, i.v.)
    References

    Br J Pharmacol. 1999 Sep;128(2):403-11; Cancer Res. 2001 Jan 15;61(2):749-58.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Tariquidar
    The effect of modulator on the steady-state accumulation of [3H]-vinblastine (100 nM) and [3H]-paclitaxel (1 μM) was measured in CHrB30 cells at 37°C as described in Methods. Br J Pharmacol. 1999 Sep;128(2):403-11.
     
    Tariquidar
    The effect of XR9576, GF120918, XR9051 and vanadate on the ATPase activity of P-gp-containing CHrB30 membranes (1 μg). Br J Pharmacol. 1999 Sep;128(2):403-11.
     
    Tariquidar
    Saturation isotherms of [3H]-XR9576, [3H]-vinblastine and [3H]-paclitaxel binding to CHrB30 membranes. Br J Pharmacol. 1999 Sep;128(2):403-11.

    Tariquidar

    Tariquidar

    Tariquidar


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