Zosuquidar
Based on 16 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 167354-41-8
- Formula: C32H31F2N3O2
- Molecular Weight:527.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
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Publications Citing Use of MedChemExpress (MCE) Zosuquidar
More- Cancer Cell. 2017 Apr 10;31(4):501-515.e8. [Abstract]
- Adv Sci (Weinh). 2025 Aug 4:e04680. [Abstract]
- Crit Rev Anal Chem. 2022;52(7):1557-1571. [Abstract]
- Blood Adv. 2020 Oct 27;4(20):5062-5077. [Abstract]
- Pharmaceutics. 2021 Apr 15;13(4):559. [Abstract]
- Antiviral Res. 2021 Sep:193:105124. [Abstract]
- Viruses. 2020 Aug 17;12(8):901. [Abstract]
- Drug Metab Dispos. 2017 May;45(5):449-456. [Abstract]
- J Pharm Biomed Anal. 2012 Jul;66:232-9. [Abstract]
- Biomed Res Int. 2020 Nov 29;2020:8878158. [Abstract]
- Biomed Res Int. 2014;2014:850493. [Abstract]
- Biochem Biophys Res Commun. 2021 Jun 25:559:222-229. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Aug 15:1092:72-81. [Abstract]
- Exp Ther Med. 2021 Feb;21(2):128. [Abstract]
- bioRxiv. 2024 November 03.
- Biomed Pharmacother. 2020 Sep;129:110506. [Abstract]
Customer Validation & Images
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Others
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Others
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Cell Proliferation/Viability Assay
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| SW-620 | IC50 |
0.059 μM
Compound: Zosuquidar
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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)
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[PMID: 34723530] |
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.
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Cell Line:K562 and HL60 cells
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Concentration:0.3 μM
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Incubation Time:48 hours
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Result:Enhanced the cytotoxicity of DNR (substrates for P-glycoproteins) in K562/DOX cells more than 45.5-fold.
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Cell Line:CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells
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Concentration:5-16 μM
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Incubation Time:72 hours
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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.
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.
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Animal Model:Mice implanted with P388/ADR tumors[1]
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Dosage:30, 10, 3, or 1 mg/kg
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Administration:Intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 days
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Result:Exihibited a significantly increased survival compared to the group treated with Doxorubicin alone (P<0.001).
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Animal Model:Mice implanted with P388 or P388/ADR murine leukemia cells[1]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection; 30 mg/kg; once daily; 5 days
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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).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 167354-41-8
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Appearance Solid
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Molecular Weight 527.60
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Formula C32H31F2N3O2
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Color Off-white to light yellow
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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
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Synonyms
RS 33295-198; LY-335979
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (16)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Eradication of Tumors through Simultaneous Ablation of CD276/B7-H3-Positive Tumor Cells and Tumor Vasculature. [Abstract]2017 Apr 10;31(4):501-515.e8. PMID: 28399408 -
Adv Sci (Weinh)
Fusidic Acid Reverses Chemoresistance in Breast Cancer via Targeting DDX6 to Downregulate GSK-3β/β-Catenin Signaling. [Abstract]2025 Aug 4:e04680. PMID: 40757496 -
Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566 -
Blood Adv
Clinical MDR1 inhibitors enhance Smac-mimetic bioavailability to kill murine LSCs and improve survival in AML models. [Abstract]2020 Oct 27;4(20):5062-5077. PMID: 33080008
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.
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Pharmaceutics
2021 Apr 15;13(4):559. PMID: 33921129
Zosuquidar purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2021 Apr 15;13(4):559. [Abstract]
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. [Abstract]
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.
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Antiviral Res
2021 Sep:193:105124. PMID: 34197862 -
Viruses
Combinatorial Treatment of Birinapant and Zosuquidar Enhances Effective Control of HBV Replication In Vivo. [Abstract]2020 Aug 17;12(8):901. PMID: 32824616 -
Drug Metab Dispos
Correlation between Membrane Protein Expression Levels and Transcellular Transport Activity for Breast Cancer Resistance Protein. [Abstract]2017 May;45(5):449-456. PMID: 28209803 -
J Pharm Biomed Anal
Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. [Abstract]2012 Jul;66:232-9. PMID: 22472186
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.
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Biomed Res Int
A Novel Cryptococcal Meningitis Therapy: The Combination of Amphotericin B and Posaconazole Promotes the Distribution of Amphotericin B in the Brain Tissue. [Abstract]2020 Nov 29;2020:8878158. PMID: 33313322 -
Biomed Res Int
An in vivo microdialysis study of FLZ penetration through the blood-brain barrier in normal and 6-hydroxydopamine induced Parkinson's disease model rats. [Abstract]2014;2014:850493. PMID: 25045708 -
Biochem Biophys Res Commun
The study of Raddeanin A cerebrovascular endothelial cell trafficking through P-glycoprotein. [Abstract]2021 Jun 25:559:222-229. PMID: 33962209 -
J Chromatogr B Analyt Technol Biomed Life Sci
Microdialysis combined with RRLC-MS/MS for the pharmacokinetics of two major alkaloids of Bi qi capsule and the potential roles of P-gp and BCRP on their penetration. [Abstract]2018 Aug 15:1092:72-81. PMID: 29883892 -
Exp Ther Med
Silencing GnT-V reduces oxaliplatin chemosensitivity in human colorectal cancer cells through N-glycan alteration of organic cation transporter member 2. [Abstract]2021 Feb;21(2):128. PMID: 33376510 -
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Biomed Pharmacother
Interplay of drug transporters P-glycoprotein (MDR1), MRP1, OATP1A2 and OATP1B3 in passage of maraviroc across human placenta. [Abstract]2020 Sep;129:110506. PMID: 32768979
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.
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. A H Dantzig, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9. [Content Brief]
[2]. Ruoping Tang, et al. Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML). BMC Cancer. 2008 Feb 13;8:51. [Content Brief]
[3]. Larry D Cripe, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. 2010 Nov 18;116(20):4077-85. [Content Brief]
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 |
Zosuquidar Related Classifications
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