Tariquidar dihydrochloride

Cat. No. 5757

Tariquidar dihydrochloride C38H38N4O6.2HCl

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Chemical Name: N-[2-[[[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarbxamide dihydrochloride

Biological Activity

Potent P-glycoprotein (P-gp) inhibitor (IC50 = 5.1 nM). Reverses drug resistance in multiple MDR cell lines. Acts as a substrate for breast cancer resistance protein (BCRP) at low concentrations and acts as an inhibitor of BCRP when used at >100 nM concentration. Potentiates the cytotoxic effects of doxorubicin (Cat. No. 2252) and mitoxantrone (Cat. No. 4250) in vitro.

Technical Data

Soluble to 100 mM in DMSO
>98 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Loo et al (2015) Mapping the binding site of the inhibitor Tariquidar that stabilizes the first transmembrane domain of P-glycoprotein. J.Biol.Chem. 290 29389. PMID: 26507655.

Kannan et al (2011) The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2). ACS Chem.Neurosci. 2 82. PMID: 22778859.

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Keywords: Tariquidar dihydrochloride, supplier, Potent, P-glycoprotein, P-gp, inhibitors, inhibits, multidrug, resistance, MDR, breast, cancer, resistant, protein, BCRP, substrates, cytotoxic, abcb1, atp, binding, cassette, 206873-63-4, Tocris Bioscience, Multidrug Transporter Inhibitor products

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