GLPBio

Zosuquidar

Catalog No.: GC16672Purity:>98.00%
COASDSData Sheet
Zosuquidar is a novel and potent P-glycoprotein (P-gp; Ki=59nM) inhibitor and multidrug resistance (MDR) modulator.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.

Zosuquidar
Cas No.: 167354-41-8
1mgIn Stock
$30.00
1
5mgIn Stock
$95.00
1
10mgIn Stock
$144.00
1
50mgIn Stock
$513.00
1
100mgIn Stock
$855.00
1
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    Nature
    641, 529–536 (2025)
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    628, 630–638 (2024)
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    388(6745) (2025)
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    387(6739) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Descripción (Description)

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.

Protocolo (Protocol)

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:
[1] 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.
[2] 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.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
167354-41-8
Nombre químico
(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
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
Fórmula molecular
C32H31F2N3O2
Peso molecular
527.6
Solubilidad
Soluble in DMSO
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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