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: 99.79%
COA Handling Instructions

Molarity Calculator

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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
5 mg USD 90 In-stock
10 mg USD 130 In-stock
50 mg USD 320 In-stock
100 mg USD 480 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 15 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    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: 99.79%

    COA (254 KB) LCMS (267 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.

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    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

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Zosuquidar trihydrochloride
    Cat. No.:
    HY-50671
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.