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

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

Cat. No.: HY-50671 Purity: 99.50%
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Handling Instructions Technical Support

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

Zosuquidar trihydrochloride Chemical Structure

CAS No. : 167465-36-3

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Zosuquidar trihydrochloride:

Zosuquidar trihydrochloride Related Antibodies

Top Publications Citing Use of Products

    Zosuquidar trihydrochloride purchased from MedChemExpress. 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].

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

    Zosuquidar trihydrochloride Related Antibodies

    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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    FC1([C@H]2[C@@H]1C3=C([C@@H](C4=CC=CC=C42)N5CCN(CC5)C[C@H](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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

    • Protocol 1

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.50%

    SDS (393 KB)

    COA (254 KB) HNMR (281 KB) RP-HPLC (242 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.5699 mL 7.8494 mL 15.6988 mL 39.2471 mL
    H2O 5 mM 0.3140 mL 1.5699 mL 3.1398 mL 7.8494 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Zosuquidar trihydrochloride Related Classifications

    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.

    Keywords:

    Zosuquidar trihydrochloride167465-36-3RS 33295-198 trihydrochloride LY-335979 trihydrochlorideP-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243anti-tumor activityacute myelogenous leukemiaAMLK562HL60CCRF-CEMCEM/VLB100P388P388/ADRMCF7MCF7/ADR27802780ADUCLA-P3UCLA-P3.003VLBInhibitorinhibitorinhibit

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