Zosuquidar (LY335979) 3HCl

Catalog No.S1481 Synonyms: RS 33295-198 (D06387) 3HCl

Zosuquidar (LY335979) 3HCl Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 430 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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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.

    Effect of P-gp expression on cell survival and proliferation of DNR and Zosuquidar(ZSQ) treated cells.

    Pharmacol Res 2013 67(1), 79-83. 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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Biological Activity

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.
Targets
P-gp [1]
(Cell-free assay)
60 nM(Ki)
In vitro

LY335979 competitively inhibits equilibrium binding of [3H]vinblastine to Pgp by blocking [3H]azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes. [1] 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. [1] 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. [2] A latest paper indicates that LY335979 completely inhibits apically directed transport of (Z)-endoxifen in the ABCB1-transduced cells. [3]

In vivo

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: CEM/VLB100, P388/ADR, MCF7/ADR, 2780AD, and UCLA-P3.OO3VLB cells
  • Concentrations: 0.05 μM to 5 μM
  • Incubation Time: 72 hours
  • Method: Cell viability is determined using a modified 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction method. Cells are harvested during logarithmic growth phase, and seeded in 96-well plates. The cells are then cultured for 72 hours in the presence of oncolytics with or without modulators. MCF-7 and MCF-7/ADR cells are incubated 24 hours before the addition of the drug with and without the LY335979. LY335979 is prepared as 2 mM DMSO stocks and added to wells to give final concentrations ranging from 0.05 to 5 μM. After 72 hours, 20 μL of freshly prepared 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (5 mg/mL in Dulbecco's PBS) is added to each well and incubated for 4 hours in a 37 °C incubator containing 5% CO2. Cells are pelleted in a Sorvall RT6000B centrifuge, 70 μL of medium is carefully removed from each well, and 100 μL of 2-propanol/0.04 N HC1 is added. Cells are resuspended 5-10 times with a Multipipettor or until no particulate matter is visible. Plates are immediately read on a Titertek Multiskan MCC/340 microplate reader Flow Laboratories with a test wavelength of 570 nm and a reference wavelength of 630 nm. Controls are measured in quadruplicate and modulators are measured in duplicate. Cytotoxicity analyses are also performed using the CeliTiter 96 AQueous assay kit.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: P388 or P388/ADR cells are implanted by i.p. injection into female BDF1 mice.
  • Formulation: LY335979 is dissolved in 5% mannitol.
  • Dosages: ≤30 mg/kg
  • Administration: Administered via i.p. and i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (156.98 mM)
Water 23 mg/mL (36.1 mM)
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 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.

Chemical Information

Molecular Weight 636.99
Formula

C32H31F2N3O2.3HCl

CAS No. 167465-36-3
Storage powder
in solvent
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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P-gp Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID