Tariquidar dihydrochloride
Based on 57 publication(s) in Google Scholar
Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
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- No. CAS: 1992047-62-7
- Fòrmula: C38H40Cl2N4O6
- Peso molecular:719.65
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Almacenamiento:
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Tariquidar dihydrochloride
More- Cell. 2023 Dec 7;186(25):5500-5516.e21. [Abstract]
- Cancer Res. 2026 May 27:10.1158/0008-5472.CAN-25-5172. [Abstract]
- Sci Bull. 2016 Apr;61(7):552-560.
- J Control Release. 2022 Sep:349:109-117. [Abstract]
- J Control Release. 2022 Feb:342:44-52. [Abstract]
- Small. 2020 Nov;16(44):e2004172. [Abstract]
- Cell Death Discov. 2021 Aug 5;7(1):204. [Abstract]
- Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]
- Phytother Res. 2026 Apr;40(4):1935-1950. [Abstract]
- Crit Rev Anal Chem. 2022;52(7):1557-1571. [Abstract]
- Commun Chem. 2024 Jul 13;7(1):158. [Abstract]
- Pharmaceutics. 2021 Feb 26;13(3):306. [Abstract]
- Eur J Med Chem. 2018 Mar 10:147:7-20. [Abstract]
- Eur J Med Chem. 2017 Feb 15:127:586-598. [Abstract]
- RSC Adv. 2016,6, 69083-69093.
- Hepatol Commun. 2024 May 2;8(5):e0437. [Abstract]
- Mar Drugs. 2024 Aug 30;22(9):396. [Abstract]
- Eur J Pharmacol. 2024 Apr 15:969:176431. [Abstract]
- Mar Drugs. 2023 Mar 14;21(3):178. [Abstract]
- Pharmaceuticals (Basel). 2023 Feb 24;16(3):349. [Abstract]
- Mar Drugs. 2023 Jan 14;21(1):54. [Abstract]
- Mar Drugs. 2022 Nov 25;20(12):738. [Abstract]
- Mar Drugs. 2022 Sep 23;20(10):597. [Abstract]
- Int J Mol Sci. 2026 Mar 11;27(6):2587. [Abstract]
- Int J Mol Sci. 2023 Mar 10;24(6):5298. [Abstract]
- Int J Mol Sci. 2022 Nov 29;23(23):14948. [Abstract]
- J Drug Deliv Sci Technol. May 2022, 103323.
- Eur J Pharm Sci. 2019 Jan 15:127:319-329. [Abstract]
- Sci Rep. 2022 Aug 9;12(1):13570. [Abstract]
- Mol Pharm. 2021 Jan 4;18(1):416-428. [Abstract]
- Mol Pharm. 2020 Sep 8;17(9):3477-3486. [Abstract]
- Mol Pharm. 2019 Mar 4;16(3):1282-1293. [Abstract]
- Sci Rep. 2017 Dec 22;7(1):18069. [Abstract]
- J Cereb Blood Flow Metab. 2021 Jul;41(7):1634-1646. [Abstract]
- J Cereb Blood Flow Metab. 2020 Jan;40(1):150-162. [Abstract]
- J Cereb Blood Flow Metab. 2016 Aug;36(8):1412-23. [Abstract]
- ACS Chem Neurosci. 2025 Sep 3;16(17):3340-3353. [Abstract]
- Langmuir. 2015 May 12;31(18):5115-22. [Abstract]
- Antiviral Res. 2021 Sep:193:105124. [Abstract]
- Antimicrob Agents Chemother. 2015 Nov 30;60(2):946-54. [Abstract]
- Pharm Res. 2017 Jan;34(1):148-160. [Abstract]
- J Nat Prod. 2022 Dec 23;85(12):2746-2752. [Abstract]
- J Nanopart Res. (2018) 20:176.
- Nucl Med Biol. 2018 May:60:29-36. [Abstract]
- PLoS One. 2026 Jan 21;21(1):e0341445. [Abstract]
- PLoS One. 2017 Sep 15;12(9):e0183662. [Abstract]
- Mol Imaging Biol. 2019 Apr;21(2):257-268. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):599-606. [Abstract]
- Xenobiotica. 2020 Mar;50(3):354-362. [Abstract]
- bioRxiv. 2025 Sep 20.
- bioRxiv. 2025 Jun 24:2025.06.18.660465. [Abstract]
- Res Sq. 2025 May 16.
- Research Square Preprint. 2024 Feb 6.
- Research Square Print. 2022 Jul.
- RWTH Aachen University. 2021 Oct.
- Research Square Preprint. 2021 Mar.
- J Biomed Nanotechnol. 2018 Oct 1;14(10):1705-1718. [Abstract]
Customer Validation & Images
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Actividad biológica
Kd: 5.1 nM (P-gp)[1]
Tariquidar (XR9576) is a potent modulator of P-gp mediated [3H]-Vinblastine and [3H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CHrB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC50=487±50 nM). [3H]-Tariquidar binds to CHrB30 membranes with the highest affinity (Kd=5.1±0.9 nM, n=7) and a binding capacity (Bmax) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [3H]-Vinblastine is increased in a dose-dependent fashion by the modulators Tariquidar (EC50=487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC50 value of 43±9 nM[1]. Tariquidar (XR9576) potentiates the cytotoxicity of several drugs including Doxorubicin, Paclitaxel, Etoposide, and Vincristine; complete reversal of resistance is achieved in the presence of 25-80 nM XR9576. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [3H]Azidopine implying a direct interaction with the protein[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1992047-62-7
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Peso molecular 719.65
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Fòrmula C38H40Cl2N4O6
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SMILES
[H]Cl.[H]Cl.O=C(C1=CC2=CC=CC=C2N=C1)NC3=CC(OC)=C(OC)C=C3C(NC4=CC=C(CCN5CC6=C(C=C(OC)C(OC)=C6)CC5)C=C4)=O
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Synonyms
XR9576 dihydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (57)
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Journal Impact Factor
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Most Recent
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Cell
2023 Dec 7;186(25):5500-5516.e21. PMID: 38016470
Tariquidar dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell. 2023 Dec 7;186(25):5500-5516.e21. [Abstract]
Survival curves of mice under SD (SR means 48 h of recovery after SD) with i.p. administration of tariquidar (n = 5) or vehicle (n = 5).
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Cancer Res
Targeted KRASG12V Degradation in vivo Elicits Lung Adenocarcinoma Regression with Subsequent Relapse from Dysregulated Proteolysis. [Abstract]2026 May 27:10.1158/0008-5472.CAN-25-5172. PMID: 42200804 -
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J Control Release
2022 Sep:349:109-117. PMID: 35798092 -
J Control Release
2022 Feb:342:44-52. PMID: 34971693 -
Small
Active Transportation of Liposome Enhances Tumor Accumulation, Penetration, and Therapeutic Efficacy. [Abstract]2020 Nov;16(44):e2004172. PMID: 33030305
Tariquidar dihydrochloride purchased from MedChemExpress. Usage Cited in: Small. 2020 Nov;16(44):e2004172. [Abstract]
In vitro tumor penetration of the DOX-loaded liposomes in BxPC3 MTS. The BxPC3 MTS were prestained with or without a Pg-p inhibitor Tariquidar (10 nM) for 3 h. Subsequently, the MTS were cultured with DOX-loaded liposomes for 6 h. The MTS were visualized using CLSM in Z-stacks with 25 µm intervals. DOX (red).
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Cell Death Discov
Compound 968 reverses adriamycin resistance in breast cancer MCF-7ADR cells via inhibiting P-glycoprotein function independently of glutaminase. [Abstract]2021 Aug 5;7(1):204. PMID: 34354052
Tariquidar dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Aug 5;7(1):204. [Abstract]
MCF-7ADR cells were treated with ADR (2μM) alone or together with Tariquidar (TQ; 0.5 μM) for 48h. Cell viability was detected using the CCK8 assays.
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Antioxidants (Basel)
The Long-Term DEHP Exposure Confers Multidrug Resistance of Triple-Negative Breast Cancer Cells through ABC Transporters and Intracellular ROS. [Abstract]2021 Jun 11;10(6):949. PMID: 34208283
Tariquidar dihydrochloride purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]
Tariquidar (1.5 μM; 72 h). Western blotting results show the specific inhibition of both MRP1/ABCC1 and MDR1/ABCB1 after tariquidar treatment for 72 h in both control and DEHP-exposed MDA-MB-231 clones.
Tariquidar dihydrochloride purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]
Tariquidar (1.5 μM; 2 h). Enhanced Dox accumulation was observed following 2 h of Tariquidar pretreatment in DEHP-exposed MDA-MB-231 clones #1 and #2, analyzed by a BD Accuri TW C6 flow cytometer.
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Phytother Res
20(R)-Ginsenoside Rg3 Suppresses P-Glycoprotein-Mediated Multidrug Resistance in A549/Taxol Cells by Targeting MDM2-IκB-α Signaling Axis. [Abstract]2026 Apr;40(4):1935-1950. PMID: 41630373 -
Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566 -
Commun Chem
2024 Jul 13;7(1):158. PMID: 39003409 -
Pharmaceutics
Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression. [Abstract]2021 Feb 26;13(3):306. PMID: 33652886 -
Eur J Med Chem
Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents. [Abstract]2018 Mar 10:147:7-20. PMID: 29421572 -
Eur J Med Chem
N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy. [Abstract]2017 Feb 15:127:586-598. PMID: 28113128 -
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Hepatol Commun
Inhibition of the transmembrane transporter ABCB1 overcomes resistance to doxorubicin in patient-derived organoid models of HCC. [Abstract]2024 May 2;8(5):e0437. PMID: 38696353 -
Mar Drugs
Stonikacidin A, an Antimicrobial 4-Bromopyrrole Alkaloid Containing L-Idonic Acid Core from the Northwestern Pacific Marine Sponge Lissodendoryx papillosa. [Abstract]2024 Aug 30;22(9):396. PMID: 39330277 -
Eur J Pharmacol
Suppression of hypoxia-induced CAV1 autophagic degradation enhances nanoalbumin-paclitaxel transcytosis and improves therapeutic activity in pancreatic cancer. [Abstract]2024 Apr 15:969:176431. PMID: 38395374 -
Mar Drugs
New Bioactive β-Resorcylic Acid Derivatives from the Alga-Derived Fungus Penicillium antarcticum KMM 4685. [Abstract]2023 Mar 14;21(3):178. PMID: 36976227 -
Pharmaceuticals (Basel)
Functionalized Lipid Nanocarriers for Simultaneous Delivery of Docetaxel and Tariquidar to Chemoresistant Cancer Cells. [Abstract]2023 Feb 24;16(3):349. PMID: 36986449 -
Mar Drugs
New Marine Fungal Deoxy-14,15-Dehydroisoaustamide Resensitizes Prostate Cancer Cells to Enzalutamide. [Abstract]2023 Jan 14;21(1):54. PMID: 36662227 -
Mar Drugs
New Guanidine Alkaloids Batzelladines O and P from the Marine Sponge Monanchora pulchra Induce Apoptosis and Autophagy in Prostate Cancer Cells. [Abstract]2022 Nov 25;20(12):738. PMID: 36547885 -
Mar Drugs
Cytotoxic N-Methylpretrichodermamide B Reveals Anticancer Activity and Inhibits P-Glycoprotein in Drug-Resistant Prostate Cancer Cells. [Abstract]2022 Sep 23;20(10):597. PMID: 36286421 -
Int J Mol Sci
2026 Mar 11;27(6):2587. PMID: 41898448 -
Int J Mol Sci
Identification and Empiric Evaluation of New Inhibitors of the Multidrug Transporter P-Glycoprotein (ABCB1). [Abstract]2023 Mar 10;24(6):5298. PMID: 36982374 -
Int J Mol Sci
Salvage Chemotherapy with Cisplatin, Ifosfamide, and Paclitaxel in Aggressive Variant of Metastatic Castration-Resistant Prostate Cancer. [Abstract]2022 Nov 29;23(23):14948. PMID: 36499277 -
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Eur J Pharm Sci
Population pharmacokinetic modeling to establish the role of P-glycoprotein on ciprofloxacin distribution to lung and prostate following intravenous and intratracheal administration to Wistar rats. [Abstract]2019 Jan 15:127:319-329. PMID: 30423435 -
Sci Rep
New diterpenes from the marine sponge Spongionella sp. overcome drug resistance in prostate cancer by inhibition of P-glycoprotein. [Abstract]2022 Aug 9;12(1):13570. PMID: 35945234 -
Mol Pharm
Pharmacokinetic Modeling of ( R)-[11C]verapamil to Measure the P-Glycoprotein Function in Nonhuman Primates. [Abstract]2021 Jan 4;18(1):416-428. PMID: 33315404 -
Mol Pharm
Pharmacokinetic Modeling of [18F]MC225 for Quantification of the P-Glycoprotein Function at the Blood-Brain Barrier in Non-Human Primates with PET. [Abstract]2020 Sep 8;17(9):3477-3486. PMID: 32787277 -
Mol Pharm
Inhibition of ABCB1 and ABCG2 at the Mouse Blood-Brain Barrier with Marketed Drugs To Improve Brain Delivery of the Model ABCB1/ABCG2 Substrate [11C]erlotinib. [Abstract]2019 Mar 4;16(3):1282-1293. PMID: 30694684 -
Sci Rep
LUCS (Light-Up Cell System), a universal high throughput assay for homeostasis evaluation in live cells. [Abstract]2017 Dec 22;7(1):18069. PMID: 29273711 -
J Cereb Blood Flow Metab
Complete inhibition of ABCB1 and ABCG2 at the blood-brain barrier by co-infusion of erlotinib and tariquidar to improve brain delivery of the model ABCB1/ABCG2 substrate [11C]erlotinib. [Abstract]2021 Jul;41(7):1634-1646. PMID: 33081568 -
J Cereb Blood Flow Metab
Age dependency of cerebral P-glycoprotein function in wild-type and APPPS1 mice measured with PET. [Abstract]2020 Jan;40(1):150-162. PMID: 30354871 -
J Cereb Blood Flow Metab
Regulation of P-glycoprotein expression in brain capillaries in Huntington's disease and its impact on brain availability of antipsychotic agents risperidone and paliperidone. [Abstract]2016 Aug;36(8):1412-23. PMID: 26661162 -
ACS Chem Neurosci
2025 Sep 3;16(17):3340-3353. PMID: 40815164 -
Langmuir
Self-assembled polymer/inorganic hybrid nanovesicles for multiple drug delivery to overcome drug resistance in cancer chemotherapy. [Abstract]2015 May 12;31(18):5115-22. PMID: 25927163 -
Antiviral Res
2021 Sep:193:105124. PMID: 34197862 -
Antimicrob Agents Chemother
Simultaneous Semimechanistic Population Analyses of Levofloxacin in Plasma, Lung, and Prostate To Describe the Influence of Efflux Transporters on Drug Distribution following Intravenous and Intratracheal Administration. [Abstract]2015 Nov 30;60(2):946-54. PMID: 26621623 -
Pharm Res
Tumor Targeting Synergistic Drug Delivery by Self-Assembled Hybrid Nanovesicles to Overcome Drug Resistance. [Abstract]2017 Jan;34(1):148-160. PMID: 27738951 -
J Nat Prod
Meroantarctines A-C, Meroterpenoids with Rearranged Skeletons from the Alga-Derived Fungus Penicillium antarcticum KMM 4685 with Potent p-Glycoprotein Inhibitory Activity. [Abstract]2022 Dec 23;85(12):2746-2752. PMID: 36413729 -
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Nucl Med Biol
A new method measuring the interaction of radiotracers with the human P-glycoprotein (P-gp) transporter. [Abstract]2018 May:60:29-36. PMID: 29529532 -
PLoS One
RIPK2 induces docetaxel resistance in prostate cancer through the NF-κB/P-gp signaling pathway. [Abstract]2026 Jan 21;21(1):e0341445. PMID: 41563982 -
PLoS One
Inflammatory cytokine production in tumor cells upon chemotherapy drug exposure or upon selection for drug resistance. [Abstract]2017 Sep 15;12(9):e0183662. PMID: 28915246 -
Mol Imaging Biol
SNAPshots of the MCHR1: a Comparison Between the PET-Tracers [18F]FE@SNAP and [11C]SNAP-7941. [Abstract]2019 Apr;21(2):257-268. PMID: 29948643 -
Eur J Drug Metab Pharmacokinet
Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration. [Abstract]2018 Oct;43(5):599-606. PMID: 29616423 -
Xenobiotica
The potential role of human multidrug resistance protein 1 (MDR1) and multidrug resistance-associated protein 2 (MRP2) in the transport of Huperzine A in vitro. [Abstract]2020 Mar;50(3):354-362. PMID: 31132291 -
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bioRxiv
2025 Jun 24:2025.06.18.660465. PMID: 40666929 -
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J Biomed Nanotechnol
Folate-Targeted Redox-Responsive Polymersomes Loaded with Chemotherapeutic Drugs and Tariquidar to Overcome Drug Resistance. [Abstract]2018 Oct 1;14(10):1705-1718. PMID: 30041718
Protocolo
Cells (EMT6 AR1.0 8×102/well; A2780 5×103/well; 2780AD 6×103/well) are seeded into 96-well plates. After ~4 h, varying concentrations of Tariquidar are added, and cells are incubated for an additional 4 days (EMT6 AR1.0) or 6 days (2780AD) before quantification of cell growth and calculation of IC10 values (concentration resulting in 10% inhibition of cell growth)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
MC26 tumor slurry is implanted s.c. in BALB/c mice (day 0). The animals are then randomized, 24 h later, into groups of 15-18 and treated once with various regimens. Tariquidar or vehicle is administered either i.v. via a lateral tail vein or p.o. with Doxorubicin (5 mg/kg) or vehicle i.v. The modulator is administered either i.v. at 2-4 mg/kg (10 mL/kg) at the same time as Doxorubicin or p.o. at 2-8 mg/kg (10 mL/kg) 1 h before the Cytotoxic drug. GG918 is administered p.o. 1 h before doxorubicin. All of the animals are weighed twice weekly. The animals are killed by cervical dislocation on day 14, and the tumors are excised and weighed. The data are analyzed by Student’s t test.
Rats[2]
Male CD rats (3 animals per time point) are dosed i.v. with paclitaxel alone [15 min infusion at 10 mg/kg in Tween 80:ethanol:5% dextrose (5:10:85% v/v/v)] or in combination with Tariquidar (10 mg/kg). Tariquidar is administered as a bolus (i.v.) dose 15 min before infusion of Paclitaxel. Blood samples are collected by cardiac puncture using heparinized syringes at various times between 0.083 and 48 h and are centrifuged to prepare plasma, which is stored at −20°C until analysis. Paclitaxel concentration in plasma samples is measured by a LC-MS/MS assay.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
Referencias
[1]. Martin C, et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol, 1999, 128(2), 403-411. [Content Brief]
[2]. Mistry P, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res, 2001, 61(2), 749-758. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tariquidar dihydrochloride Related Classifications
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