Zosuquidar (LY335979) 3HCl
Catalog No.S1481 Synonyms: RS 33295-198 (D06387) 3HCl
Molecular Weight(MW): 636.99
Zosuquidar (LY335979) 3HCl is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. Phase 3.
Cited by 7 Publications
3 Customer Reviews
Inhibition of doxorubicin compartmentalization by combined treatment with inhibitors of Abcb1 and Abcc1. A: The cells had been incubated with vehicle or 1 uM zosuquidar plus 15 uM MK571 (ZO/MK), before addition of 1 uM doxorubicin (Doxo) and further cultivation in serum-free medium for 16 h. Shown are typical images of doxorubicin (red) and Hoechst 33342 (blue) fluorescence in Sgpl1+/+ - and Sgpl1-/- -MEFs after treatment as indicated. Two images of Sgpl1-/- -cells treated with doxorubicin plus ZO/MK were selected to show the range of the cellular response. B: Hoechst 33342 staining in MEFs that had been incubated with ZO/MK in the absence of doxorubicin.
J Lipid Res 2014 10.1194/jlr.M052761. Zosuquidar (LY335979) 3HCl purchased from Selleck.
Effects of zosuquidar treatment on Zn uptake and accumulation in T. japonicus whole bodies for 24 h. Upper part in each picture represents Newport Green™ PDX Acetoxymethyl Ether, and lower parts merged images. (a-c) T. japonicus not treated with Zn. (d-f) T. japonicus treated with Zn. (g-i) T. japonicus treated with Zn and zosuquidar.
Aquat Toxicol 2014 156C, 135-147. Zosuquidar (LY335979) 3HCl purchased from Selleck.
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|Description||Zosuquidar (LY335979) 3HCl is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. Phase 3.|
LY335979 competitively inhibits equilibrium binding of [3H]vinblastine to Pgp by blocking [3H]azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes.  LY335979 alone shows the cytotoxicity to drug-sensitive and MDR cell lines with IC50 ranging from 6 μM-16 μM and produces its ability to completely reverse the resistance of the oncolytics (vinblastine, doxorubicin, or etoposide) to the MDR cell lines P388/ADR, MCF7/ADR, 2780AD, or UCLA-P3.003VLB at concentration of 0.1 and 0.5 μM.  LY335979 significantly restores drug sensitivity in P-gp-expressing leukemia cell lines including K562/HHT40, K562/HHT90, K562/DOX and HL60/DNR, and enhances the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AML blasts with active P-gp.  A latest paper indicates that LY335979 completely inhibits apically directed transport of (Z)-endoxifen in the ABCB1-transduced cells. 
ATPase Assay :P-Glycoprotein ATPase activity is measured by the liberation of inorganic phosphate from ATP. The assay is measured in a 96-well plate for 90 min at 37 °C. Membranes (8 μg-10 μg protein) are incubated in a total volume of 100 μL of buffer A containing 5 mM sodium azide, 1 mM ouabain, 1 mM EGTA, 3 mM ATP, an ATP regenerating system composed of 5 mM phosphoenolpyruvate, and 3.6 units/mL pyruvate kinase in the presence and absence of 1 mM sodium vanadate. Pgp-ATPase activity is defined as the vanadate-sensitive portion of the total ATPase activity. Plates are read 3 minutes after the addition of the detection solution. The absorbance is measured at 690 nm by a microtiter dish reader. A phosphate standard curve is used to calculate the μmol of phosphate formed. Samples are measured in triplicate.
|In vitro||DMSO||100 mg/mL (156.98 mM)|
|Water||23 mg/mL (36.1 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||RS 33295-198 (D06387) 3HCl|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00233909||Completed||Leukemia, Myeloid||Kanisa Pharmaceuticals||October 2005||Phase 1|Phase 2|
|NCT00129168||Completed||Leukemia, Myeloid||Kanisa Pharmaceuticals||August 2005||Phase 1|Phase 2|
|NCT00046930||Completed||Leukemia|Myelodysplastic Syndromes||Eastern Cooperative Oncology Group|National Cancer Institute (NCI)|Eli Lilly and Company|Kanisa Pharmaceuticals||July 2002||Phase 3|
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