Tariquidar dihydrochloride

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Description: Potent P-glycoprotein (P-gp) inhibitor
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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity for Tariquidar dihydrochloride

Tariquidar dihydrochloride is a 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.

Compound Libraries for Tariquidar dihydrochloride

Tariquidar dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Tariquidar dihydrochloride

M. Wt 719.66
Formula C38H38N4O6.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1992047-62-7
PubChem ID 121513890
InChI Key ZJCJRGRTDKIFJJ-UHFFFAOYSA-N
Smiles O=C(C1=CC(OC)=C(OC)C=C1NC(C2=CN=C(C=CC=C3)C3=C2)=O)NC(C=C4)=CC=C4CCN5CC6=CC(OC)=C(OC)C=C6CC5.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Tariquidar dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.98 50

Preparing Stock Solutions for Tariquidar dihydrochloride

The following data is based on the product molecular weight 719.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.78 mL 13.9 mL 27.79 mL
2.5 mM 0.56 mL 2.78 mL 5.56 mL
5 mM 0.28 mL 1.39 mL 2.78 mL
25 mM 0.06 mL 0.28 mL 0.56 mL

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Product Datasheets for Tariquidar dihydrochloride

Certificate of Analysis / Product Datasheet
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References for Tariquidar dihydrochloride

References are publications that support the biological activity of the product.

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

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


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Keywords: Tariquidar dihydrochloride, 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, Multidrug, Transporters, 5757, Tocris Bioscience

Citations for Tariquidar dihydrochloride

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