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

Zosuquidar  (Synonyms: RS 33295-198; LY-335979; ゾスキダル)

製品番号: HY-15255 純度: 99.96%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 167354-41-8

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 232 在庫あり
Solution
10 mM * 1 mL in DMSO USD 232 在庫あり
Solid
5 mg $200 在庫あり
10 mg $350 在庫あり
25 mg $730 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

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カスタマーレビュー

Based on 16 publication(s) in Google Scholar

Other Forms of Zosuquidar:

Zosuquidar 関連抗体

Top Publications Citing Use of Products

    Zosuquidar purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2021 Apr 15;13(4):559.

    TPT (200 μM) accumulation after co-treatment with Zosuquidar (1 μM), Ko143 (1 μM), and the combination of both (1 μM each) in ADR and MX100 cells.

    Zosuquidar purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2021 Apr 15;13(4):559.

    Change in tumor volume after co-treatment of TPT with compounds 2 and LL347 versus TPT-only, vehicle-only, and positive controls (co-treatment with the combination of Zosuquidar (2 mg/kg) and Ko143) twice a week.

    Zosuquidar purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110506.  [Abstract]

    Effect of Mdr1 inhibitor Zosuquidar (LY, 2 μM) and control MRP1 inhibitor MK-571 (MK, 50 μM) on maraviroc accumulation in MDCKII-parental and MDCKII-MRP1 cells.

    Zosuquidar purchased from MedChemExpress. Usage Cited in: Blood Adv. 2020 Oct 27;4(20):5062-5077.  [Abstract]

    HoxA9/Meis1 AML cells were treated with 10, 100, 500, and 1000 nM reserpine, tariquidar (Tari), or zosuquidar (Zosu), with or without Bir (200 nM), for 24 hours.

    Zosuquidar 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.

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

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

    Cellular Effect
    Cell Line Type Value Description References
    SW-620 IC50
    0.059 μM
    Compound: Zosuquidar
    Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 2 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 2 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM)
    		[PMID: 34723530]
    体外実験

    Zosuquidar (0.3 μM; 48 h) treatment 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 関連抗体

    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.
    体内実験

    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).
    臨床実験
    分子量

    527.60

    分子式

    C32H31F2N3O2
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to light 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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (189.54 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 1.8954 mL 9.4769 mL 18.9538 mL
    5 mM 0.3791 mL 1.8954 mL 3.7908 mL
    10 mM 0.1895 mL 0.9477 mL 1.8954 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.96%

    COA (252 KB) HNMR (139 KB) RP-HPLC (163 KB) LCMS (235 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8954 mL 9.4769 mL 18.9538 mL 47.3844 mL
    5 mM 0.3791 mL 1.8954 mL 3.7908 mL 9.4769 mL
    10 mM 0.1895 mL 0.9477 mL 1.8954 mL 4.7384 mL
    15 mM 0.1264 mL 0.6318 mL 1.2636 mL 3.1590 mL
    20 mM 0.0948 mL 0.4738 mL 0.9477 mL 2.3692 mL
    25 mM 0.0758 mL 0.3791 mL 0.7582 mL 1.8954 mL
    30 mM 0.0632 mL 0.3159 mL 0.6318 mL 1.5795 mL
    40 mM 0.0474 mL 0.2369 mL 0.4738 mL 1.1846 mL
    50 mM 0.0379 mL 0.1895 mL 0.3791 mL 0.9477 mL
    60 mM 0.0316 mL 0.1579 mL 0.3159 mL 0.7897 mL
    80 mM 0.0237 mL 0.1185 mL 0.2369 mL 0.5923 mL
    100 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4738 mL
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    Zosuquidar Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    Zosuquidar167354-41-8RS 33295-198 LY-335979LY335979LY 335979LY-335979P-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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    製品名:
    Zosuquidar
    製品番号:
    HY-15255
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