Zosuquidar |
Catalog No.GC16672
One-Click Copy Product Info
|
Zosuquidar is a novel and potent P-glycoprotein (P-gp; Ki=59nM) inhibitor and multidrug resistance (MDR) modulator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 167354-41-8
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Zosuquidar is a novel and potent P-glycoprotein (P-gp; Ki=59nM) inhibitor and multidrug resistance (MDR) modulator. Zosuquidar can be used in research related to acute myeloid leukemia (AML) and multidrug-resistant tumors[1-4].
In vitro, Zosuquidar (10.0μM) was co-incubated with 1-(hydroxymethyl)-3,4-dimethoxy-9H-xanthen-9-one (OX6; 20.0μM) in everted intestinal sacs for 5–45 minutes. Zosuquidar blocked the OX6-induced increase in Rhodamine 123 efflux[5]. Zosuquidar (0.3μM) was co-treated with chemotherapeutic agents in P-gp-expressing leukemia cell lines (K562/HHT40, K562/HHT90, K562/DOX, HL60/DNR) and primary AML blasts for 48 hours. Zosuquidar significantly enhanced the cytotoxicity of chemotherapeutic agents and restored cellular drug sensitivity[6].
In vivo, Zosuquidar (90mg/kg; once daily) was administered orally to BALB/c nude mice bearing NCI-H292 cells for 10 days. Zosuquidar significantly reduced PD-L1 expression in tumors[7]. Zosuquidar (5mg/kg or 25mg/kg; three times a week) was combined with Birinapant (3mg/kg or 10mg/kg; administered 5 hours after the third Zosuquidar injection; once weekly) via intraperitoneal injection in hepatitis B virus (HBV)-infected C57BL/6 mice for three consecutive weeks. Zosuquidar enhanced Birinapant-mediated death of HBV-positive hepatocytes and improved the kinetics of HBV-DNA and HBsAg control[8].
References:
[1] Cripe LD, Uno H, Paietta EM, 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.
[2] Dantzig AH, Shepard RL, Cao J, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9.
[3] Fan X, Guo D, Li S, et al. Fusidic Acid Reverses Chemoresistance in Breast Cancer via Targeting DDX6 to Downregulate GSK-3β/β-Catenin Signaling. Adv Sci (Weinh). 2025 Oct;12(39):e04680.
[4] Seaman S, Zhu Z, Saha S, et al. Eradication of Tumors through Simultaneous Ablation of CD276/B7-H3-Positive Tumor Cells and Tumor Vasculature. Cancer Cell. 2017 Apr 10;31(4):501-515.e8.
[5] Martins E, Silva V, Lemos A, et al. Newly Synthesized Oxygenated Xanthones as Potential P-Glycoprotein Activators: In Vitro, Ex Vivo, and In Silico Studies. Molecules. 2019 Feb 15;24(4):707.
[6] Tang R, Faussat AM, Perrot JY, et al. Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML). BMC Cancer. 2008 Feb 13;8:51.
[7] Ding L, Guo H, Zhang J, et al. Zosuquidar Promotes Antitumor Immunity by Inducing Autophagic Degradation of PD-L1. Adv Sci (Weinh). 2024 Nov;11(41):e2400340.
[8] Morrish E, Mackiewicz L, Silke N, et al. Combinatorial Treatment of Birinapant and Zosuquidar Enhances Effective Control of HBV Replication In Vivo. Viruses. 2020 Aug 17;12(8):901.
| Cell experiment [1]: | |
Cell lines | human myeloid leukemia cell lines (K562, HL60 and their variant resistant cell lines: K562/HHT40, K562/HHT90, K562/DOX, K562/BCRP, HL60/DNR, HL60/ADR) and primary AML blasts from patients |
Preparation Method | Cells were cultured in RPMI 1640 medium supplemented with 10% fetal calf serum, penicillin, and streptomycin at 37°C, 5% CO₂. Cells were treated with escalating concentrations of chemotherapeutic agents (daunorubicin, idarubicin, mitoxantrone, semi-synthetic HHT, or gemtuzumab ozogamicin) in the presence or absence of Zosuquidar for 48 hours. Cell viability was assessed by MTT assay. |
Reaction Conditions | 0.3μM; 48 hours |
Applications | Zosuquidar completely or partially restored drug sensitivity in all P-gp-expressing leukemia cell lines tested and enhanced the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin in primary AML blasts with active P-gp. In addition, P-gp inhibition by Zosuquidar was found to be more potent than cyclosporine A in cells with highly active P-gp. |
| Animal experiment [2]: | |
Animal models | Immunocompetent male C57BL/6 mice with HBV infection induced by hydrodynamic injection (HDI) of an HBV-encoding plasmid |
Preparation Method | Zosuquidar was prepared in 2% D-mannitol, 0.015% glycine in sterile H₂O and diluted in saline solution, phosphate-buffered saline (PBS). Five days following induction of infection, mice were pre-treated by intraperitoneal (IP) injection with Zosuquidar (5mg/kg or 25mg/kg) for three days. Five hours following the last dose of Zosuquidar, birinapant (3mg/kg) was delivered by IP injection. For serial serum HBV-DNA analysis, mice were IP injected with Zosuquidar three times a week (5mg/kg or 25mg/kg) and birinapant once a week (10mg/kg) for three weeks. |
Dosage form | 5mg/kg or 25mg/kg; i.p.; three times a week for three weeks. |
Applications | The combination of birinapant and Zosuquidar was well tolerated in both HBV-replicating and healthy uninfected animals. In HBV-replicating animals, the addition of Zosuquidar to birinapant treatment increased alanine aminotransferase (ALT) levels in a dose-dependent fashion, indicating enhanced hepatocyte death. This combination treatment specifically killed hepatitis B virus core protein (HBcAg)-positive HBV-replicating liver cells. Furthermore, combined treatment of birinapant and Zosuquidar significantly reduced the time taken for animals to diminish HBV virus compared to birinapant single-agent treatment and resulted in a greater reduction in serum HBV surface antigen (HBsAg). |
References: | |
| Cas No. | 167354-41-8 | SDF | |
| Chemical Name | (2R)-1-(4-((1aR,10bS)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c][7]annulen-6-yl)piperazin-1-yl)-3-(quinolin-5-yloxy)propan-2-ol | ||
| Canonical SMILES | FC1([C@@](C2=C([H])C([H])=C([H])C([H])=C23)([H])[C@]1([H])C4=C([H])C([H])=C([H])C([H])=C4C3([H])N5C([H])([H])C([H])([H])N(C([H])([H])[C@@](C([H])([H])OC6=C([H])C([H])=C([H])C7=C6C([H])=C([H])C([H])=N7)([H])O[H])C([H])([H])C5([H])[H])F | ||
| Formula | C32H31F2N3O2 | M.Wt | 527.6 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8954 mL | 9.4769 mL | 18.9538 mL |
| 5 mM | 379.1 μL | 1.8954 mL | 3.7908 mL |
| 10 mM | 189.5 μL | 947.7 μL | 1.8954 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)