1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. Zosuquidar trihydrochloride

Zosuquidar trihydrochloride  (Synonyms: RS 33295-198 trihydrochloride; LY-335979 trihydrochloride)

Cat. No.: HY-50671 Purity: 99.79%
COA Handling Instructions

Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.

For research use only. We do not sell to patients.

Zosuquidar trihydrochloride Chemical Structure

Zosuquidar trihydrochloride Chemical Structure

CAS No. : 167465-36-3

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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Zosuquidar trihydrochloride:

Top Publications Citing Use of Products

    Zosuquidar trihydrochloride purchased from MCE. Usage Cited in: J Pharm Biomed Anal. 2012 Jul;66:232-9.  [Abstract]

    Effect of pharmacological inhibition of drug efflux transporters on brain distribution of FLZ in rats. The rats receive 35 mg/kg FLZ via tail vein injection 10 min after intravenous administration of 20 mg/kg Zosuquidar or 7.5 mg/kg ko143.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research[1][2][3].

    IC50 & Target

    Ki: 59nM (P-glycoprotein)[1].

    In Vitro

    Zosuquidar (0.3 μM; 48 h) enhances the cytotoxicity of DNR (substrates for P-glycoproteins) in P-glycoproteins active cell lines[2].
    Zosuquidar (5-16 μM; 72 h) treatment alone shows high cytotoxic concentration to drug-sensitive and MDR cell lines[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Cytotoxicity Assay[2]

    Cell Line: K562 and HL60 cells
    Concentration: 0.3 μM
    Incubation Time: 48 hours
    Result: Enhanced the cytotoxicity of DNR (substrates for P-glycoproteins) in K562/DOX cells more than 45.5-fold.

    Cell Cytotoxicity Assay[1]

    Cell Line: CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells
    Concentration: 5-16 μM
    Incubation Time: 72 hours
    Result: Showed IC50s of 6, 7, 15, 8, 7, 15, 11, 16, >5, >5 μM for CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells, respectively.
    In Vivo

    Zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) treatment shows a significant increase in life span[1].
    Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Mice implanted with P388/ADR tumors[1]
    Dosage: 30, 10, 3, or 1 mg/kg
    Administration: Intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 days
    Result: Exihibited a significantly increased survival compared to the group treated with Doxorubicin alone (P<0.001).
    Animal Model: Mice implanted with P388 or P388/ADR murine leukemia cells[1]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; 30 mg/kg; once daily; 5 days
    Result: Observed significant antitumor activity against the MDR P388/ADR cell lines when mice were treated with a combined dose of 30 mg/kg LY335979 and 1 mg/kg Doxorubicin (P=0.1).
    Clinical Trial
    Molecular Weight

    636.99

    Formula

    C32H34Cl3F2N3O2

    CAS No.
    SMILES

    FC1([[email protected]]2[[email protected]@H]1C3=C([[email protected]@H](C4=CC=CC=C42)N5CCN(CC5)C[[email protected]](COC6=C7C=CC=NC7=CC=C6)O)C=CC=C3)F.Cl.Cl.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    H2O : 5 mg/mL (7.85 mM; Need ultrasonic)

    DMSO : 1 mg/mL (1.57 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5699 mL 7.8494 mL 15.6988 mL
    5 mM 0.3140 mL 1.5699 mL 3.1398 mL
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Zosuquidar is dissolved in 20% ethanol-saline[5].

    Purity & Documentation

    Purity: 99.79%

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Zosuquidar trihydrochloride
    Cat. No.:
    HY-50671
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