A quinoline derivative and inhibitor of multidrug resistance
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Dofequidar

Item No. 30925

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[2-hydroxy-3-(5-quinolinyloxy)propyl]-1-piperazinyl]-2,2-diphenyl-ethanone
CAS Number
129716-58-1
Molecular Formula
C30H31N3O3
Formula Weight
481.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
OC(CN1CCN(C(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)CC1)COC4=CC=CC5=C4C=CC=N5
InChi Code
InChI=1S/C30H31N3O3/c34-25(22-36-28-15-7-14-27-26(28)13-8-16-31-27)21-32-17-19-33(20-18-32)30(35)29(23-9-3-1-4-10-23)24-11-5-2-6-12-24/h1-16,25,29,34H,17-22H2
InChi Key
KLWUUPVJTLHYIM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

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    10 mg

    $283

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    Product Description

    Dofequidar is a quinoline derivative and inhibitor of multidrug resistance.1,2 It inhibits P-glycoprotein in a photolabeling assay when used at a concentration of 100 μM.1 Dofequidar (10 μM) increases intracellular accumulation of [3H]-vincristine in HL-60R cells endogenously expressing the gene encoding multidrug resistance-associated protein (MRP).2 It restores susceptibility to vincristine- or doxorubicin-induced cytotoxicity in vincristine-resistant P388, vincristine-resistant K562, and doxorubicin-resistant K562 cells in a concentration-dependent manner.1 Dofequidar (80 mg/kg twice per day) increases survival in a vincristine-resistant P388 murine leukemia model compared with untreated controls when administered in combination with vincristine (Item No. 11764).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sato, W., Fukazawa, N., Nakanishi, O., et al. Reversal of multidrug resistance by a novel quinoline derivative, MS-209. Cancer Chemother. Pharmacol. 35(4), 271-277 (1995).

    2. Narasaki, F., Oka, M., Fukuda, M., et al. A novel quinoline derivative, MS-209, overcomes drug resistance of human lung cancer cells expressing the multidrug resistance-associated protein (MRP) gene. Cancer Chemother. Pharmacol. 40(5), 425-432 (1997).