Z57346765
Based on 1 publication(s) in Google Scholar
Z57346765 is an inhibitor that targets the ADP-binding pocket of PGK1, with a Kd of 20.9 μM for human PGK1, and exhibits anticancer activity. Z57346765 reduces the activity of the metabolic enzyme PGK1 during glycolysis, regulates lipid peroxidation and cancer cell proliferation, and promotes lipid peroxidation in cervical cancer cells. Z57346765 inhibits the proliferation of cervical cancer and clear cell renal cell carcinoma cells in xenograft mouse models, and induces the expression of genes associated with cell metabolism, DNA replication and cell cycle. Z57346765 is used in research related to cervical cancer, clear cell renal cell carcinoma and breast cancer.
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- Reinheit: 99.85%
- CAS. Nr.: 1016340-64-9
- Formel: C17H18N4O
- Molecular Weight:294.36
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Z57346765
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Biologische Aktivität
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PGK1 20.9 μM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | IC50 |
26.59 μM
Compound: Z57346765
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Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38354523] |
| ACHN | IC50 |
18.15 μM
Compound: Z57346765
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Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38354523] |
| HK-2 | IC50 |
49.45 μM
Compound: Z57346765
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Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38354523] |
| OS-RC-2 | IC50 |
28.64 μM
Compound: Z57346765
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Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38354523] |
Z57346765 (1 μM-100 μM; 48 h) inhibits the viability of human clear cell renal cell carcinoma (KIRC) cell lines 786-O, ACHN and OS-RC-2 in a dose-dependent manner, with mean IC50 values of 26.59, 18.15 and 28.64 μM, respectively, and exhibits low toxicity against normal HK-2 renal epithelial cells (IC50=49.45 μM)[2].
Z57346765 (5-15 μM; 10-14 days) inhibits the clonogenic proliferation of human clear cell renal cell carcinoma (KIRC) cell lines 786-O, ACHN and OS-RC-2 in a dose-dependent manner[2].
Z57346765 (20 μM; 24 h) arrests the cell cycle of human clear cell renal cell carcinoma (KIRC), alters the gene expression of OS-RC-2 clear cell renal cell carcinoma cells, and the differentially expressed genes are significantly enriched in pathways related to cell metabolism, DNA replication and cell cycle[2].
Z57346765 (20 μM; 48 h) inhibits the expression of proteins involved in cell cycle, DNA replication and proliferation signaling (cyclin B1, cyclin D1, CDK1, CDK2, MCM3, MCM5, POLD1, p-AKT, p-ERK), and upregulates the expression of PGK1 protein in human clear cell renal cell carcinoma (KIRC) cell lines 786-O, ACHN and OS-RC-2[2].
Z57346765 (15-45 μM; 48 h) enhances the sensitivity of Sorafenib (HY-10201)-resistant OS-RC-2 clear cell renal cell carcinoma (KIRC) cells to sorafenib in a dose-dependent manner, and the cell-killing effect after 48 h of combined treatment is superior to that of monotherapy[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human KIRC cell lines 786-O, ACHN, OS-RC-2; normal human renal tubular epithelial cell line HK-2
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Concentration:5, 10, 15 μM
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Incubation Time:10-14 days, with fresh compound added twice weekly
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Result:Significantly reduced clonogenic growth of KIRC cells in a dose-dependent manner, with greater inhibition observed at higher concentrations.
Caused marked inhibition of colony formation in 786-O, ACHN, and OS-RC-2 cells at 10 μM.
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Cell Line:Human KIRC cell lines 786-O, ACHN, OS-RC-2
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Concentration:20 μM
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Incubation Time:48 h
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Result:Induced prominent cell cycle arrest at the G1/S phase in all three KIRC cell lines, with increased cell population in G1 phase and decreased population in S phase.
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Cell Line:Human KIRC cell lines 786-O, ACHN, OS-RC-2
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Concentration:20 μM
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Incubation Time:48 h
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Result:Reduced protein expression of cell cycle-related genes (cyclin B1, cyclin D1, CDK1, CDK2), DNA replication-related genes (MCM3, MCM5, POLD1), and proliferation-associated phosphorylated proteins (p-AKT, p-ERK) in all three KIRC cell lines.
Increased PGK1 protein expression in treated cells.
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Cell Line:Human KIRC cell line OS-RC-2 (sorafenib-resistant model)
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Concentration:15-45 μM (Z57346765); 0-27 μM (Sorafenib)
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Incubation Time:48 h
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Result:The combination of Z57346765 and sorafenib significantly enhanced anti-tumor efficacy compared to either treatment alone.
As Z57346765 concentration increased, OS-RC-2 cell resistance to sorafenib decreased, as shown by reduced OD450 values (fewer live cells).
Z57346765 (40 mg/kg; i.p.; once daily for 16 consecutive days) significantly inhibits the growth of subcutaneous OS-RC-2 tumors in BALB/c nude mice, while the tested dose also induces detectable cardiopulmonary toxicity in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude with Kidney renal clear cell carcinoma (5-week-old, male, immunodeficient, subcutaneous inoculation of OS-RC-2 cells)[2]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:i.p.; daily; 16 days
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Result:Reduced mean tumor volume to 414.87 mm3 at 40 mg/kg. Reduced mean tumor volume to 572.68 mm3 at 20 mg/kg.
Reduced Ki-67 protein expression in tumor tissues at both 20 mg/kg and 40 mg/kg.
Increased tumor necrotic area relative to control at 40 mg/kg. Reduced body weight to 18.90 g (vs 21.34 g in controls), at 40 mg/kg.
Induced irregular cardiomyocyte morphology and thickened alveolar septa in lungs at both tested doses.
Chemical Information
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CAS. Nr. 1016340-64-9
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Appearance Solid
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Molecular Weight 294.36
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Formel C17H18N4O
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Color Off-white to light yellow
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SMILES
OCCNC1=C2C=CC=CC2=NC(NC3=CC=C(C)C=C3)=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (339.72 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (8.49 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 (8.49 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.
Reinheit & Dokumentation
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Data Sheet (283 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)
Verweise
[1]. Zhang B, et al. Downregulation of PGK1 promotes lipid peroxidation and suppresses proliferation in cervical cancer revealed by liquid-liquid phase separation-related gene signature. BMC Cancer. 2025;25(1):1269. Published 2025 Aug 5. [Content Brief]
[2]. He Y, et al. Novel inhibitors targeting the PGK1 metabolic enzyme in glycolysis exhibit effective antitumor activity against kidney renal clear cell carcinoma in vitro and in vivo. Eur J Med Chem. 2024;267:116209. [Content Brief]
[3]. Chen X, et al. Identification of a Potential PGK1 Inhibitor with the Suppression of Breast Cancer Cells Using Virtual Screening and Molecular Docking. Pharmaceuticals (Basel). 2024;17(12):1636. Published 2024 Dec 5. [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 | 3.3972 mL | 16.9860 mL | 33.9720 mL | 84.9300 mL |
| 5 mM | 0.6794 mL | 3.3972 mL | 6.7944 mL | 16.9860 mL | |
| 10 mM | 0.3397 mL | 1.6986 mL | 3.3972 mL | 8.4930 mL | |
| 15 mM | 0.2265 mL | 1.1324 mL | 2.2648 mL | 5.6620 mL | |
| 20 mM | 0.1699 mL | 0.8493 mL | 1.6986 mL | 4.2465 mL | |
| 25 mM | 0.1359 mL | 0.6794 mL | 1.3589 mL | 3.3972 mL | |
| 30 mM | 0.1132 mL | 0.5662 mL | 1.1324 mL | 2.8310 mL | |
| 40 mM | 0.0849 mL | 0.4247 mL | 0.8493 mL | 2.1233 mL | |
| 50 mM | 0.0679 mL | 0.3397 mL | 0.6794 mL | 1.6986 mL | |
| 60 mM | 0.0566 mL | 0.2831 mL | 0.5662 mL | 1.4155 mL | |
| 80 mM | 0.0425 mL | 0.2123 mL | 0.4247 mL | 1.0616 mL | |
| 100 mM | 0.0340 mL | 0.1699 mL | 0.3397 mL | 0.8493 mL |
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