Catalog Number: 5757
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
  • M.Wt:
    719.66
  • Formula:
    C38H38N4O6.2HCl
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    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.
Background References
  1. The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).
    Kannan et al.
    ACS Chem.Neurosci., 2011;2:82
  2. Mapping the binding site of the inhibitor Tariquidar that stabilizes the first transmembrane domain of P-glycoprotein.
    Loo et al.
    J.Biol.Chem., 2015;290:29389
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