A quinoline derivative and inhibitor of multidrug resistance; inhibits P-glycoprotein in a photolabeling assay at 100 μM; increases intracellular accumulation of [3H]-vincristine in HL-60R cells endogenously expressing the gene encoding MRP at 10 μM; restores susceptibility to vincristine- or doxorubicin-induced cytotoxicity in vincristine-resistant P388

Dofequidar – 5 mg

Brand:
Cayman
CAS:
129716-58-1
Storage:
-20
UN-No:
Non-Hazardous - /

Dofequidar is a quinoline derivative and inhibitor of multidrug resistance.{53975,53976} It inhibits P-glycoprotein in a photolabeling assay when used at a concentration of 100 μM.{53975} Dofequidar (10 μM) increases intracellular accumulation of [3H]-vincristine in HL-60R cells endogenously expressing the gene encoding multidrug resistance-associated protein (MRP).{53976} 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.{53975} 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).  

 

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SKU: 30925 - 5 mg Category:

Description

A quinoline derivative and inhibitor of multidrug resistance; inhibits P-glycoprotein in a photolabeling assay at 100 μM; increases intracellular accumulation of [3H]-vincristine in HL-60R cells endogenously expressing the gene encoding MRP at 10 μM; restores susceptibility to vincristine- or doxorubicin-induced cytotoxicity in vincristine-resistant P388, vincristine-resistant K562, and doxorubicin-resistant K562 cells; increases survival in a vincristine-resistant P388 murine leukemia model compared with untreated controls at 80 mg/kg twice per day when administered in combination with vincristine

Formal name: 1-[4-[2-hydroxy-3-(5-quinolinyloxy)propyl]-1-piperazinyl]-2,2-diphenyl-ethanone

Synonyms: 

Molecular weight: 481.6

CAS: 129716-58-1

Purity: ≥98%

Formulation: A solid

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