Art. -Nr.: HY-15255

Zosuquidar

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

16 Cited Publications

Kundenbewertung

Based on 16 publication(s) in Google Scholar

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

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Reinheit: 99.96%
CAS. Nr.: 167354-41-8
Formel: C₃₂H₃₁F₂N₃O₂
Molecular Weight:527.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Zosuquidar Chemical Structure

CAS. Nr.: 167354-41-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Zosuquidar (LY335979) is a P-glycoprotein (P-gp) inhibitor (K_i=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]

In Vitro

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 167354-41-8
Appearance Solid
Molecular Weight 527.60
Formel C₃₂H₃₁F₂N₃O₂
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
Synonyms

RS 33295-198; LY-335979
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (16)

All Cell Proliferation/Viability AssayOthersIn Vivo Efficacy Study

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Journal Impact Factor

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.
Pharmaceutics

Dual Inhibition of P-gp and BCRP Improves Oral Topotecan Bioavailability in Rodents. [Abstract]

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.
Antiviral Res

Valspodar limits human cytomegalovirus infection and dissemination. [Abstract]

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.
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
bioRxiv

2024 November 03.
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.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

16 Cited Publications

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Zosuquidar

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Blood Cancer Compound Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Zosuquidar

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zosuquidar

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Blood Cancer Compound Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Zosuquidar

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zosuquidar Related Classifications

HY-15255 Related Classifications