2. Metabolic Enzyme/Protease
  3. Phosphoglycerate Kinase (PGK)
  4. Z57346765

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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Z57346765

Z57346765 Chemical Structure

CAS No. : 1016340-64-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Z57346765 Related Antibodies

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1 Publications Citing Use of MCE Z57346765

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PGK1

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Description

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[1][2][3].

IC50 & Target

PGK1

20.9 μM (Kd)

Cellular Effect
Cell Line Type Value Description References
786-0 IC50
26.59 μM
Compound: Z57346765
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
[PMID: 38354523]
ACHN IC50
18.15 μM
Compound: Z57346765
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
[PMID: 38354523]
HK-2 IC50
49.45 μM
Compound: Z57346765
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
[PMID: 38354523]
OS-RC-2 IC50
28.64 μM
Compound: Z57346765
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
[PMID: 38354523]
In Vitro

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.

Z57346765 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: Human KIRC cell lines 786-O, ACHN, OS-RC-2; normal human renal tubular epithelial cell line HK-2
Concentration: 5, 10, 15 μM
Incubation Time: 10-14 days, with fresh compound added twice weekly
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.

Cell Cycle Analysis[2]

Cell Line: Human KIRC cell lines 786-O, ACHN, OS-RC-2
Concentration: 20 μM
Incubation Time: 48 h
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.

Western Blot Analysis[2]

Cell Line: Human KIRC cell lines 786-O, ACHN, OS-RC-2
Concentration: 20 μM
Incubation Time: 48 h
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.

Cell Viability Assay[2]

Cell Line: Human KIRC cell line OS-RC-2 (sorafenib-resistant model)
Concentration: 15-45 μM (Z57346765); 0-27 μM (Sorafenib)
Incubation Time: 48 h
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).
In Vivo

Z57346765 (5-45 mg/kg; single dose) significantly reduces cervical cancer tumor volume in cell-derived xenograft mouse models without causing measurable body weight loss[1].
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.

Animal Model: BALB/c nude with Kidney renal clear cell carcinoma (5-week-old, male, immunodeficient, subcutaneous inoculation of OS-RC-2 cells)[2]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; daily; 16 days
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.
Molecular Weight

294.36

Formula

C17H18N4O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OCCNC1=C2C=CC=CC2=NC(NC3=CC=C(C)C=C3)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3972 mL 16.9860 mL 33.9720 mL
5 mM 0.6794 mL 3.3972 mL 6.7944 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.85%

SDS (394 KB)

COA (250 KB)

Handling Instructions (2659 KB)
References

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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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Z573467651016340-64-9Z 57346765Z-57346765Phosphoglycerate Kinase (PGK)Phosphoglycerate KinasePGK1lipid peroxidationACHN786-OOS-RC-2kidney renal clear cell carcinomaglycolysiscervical cancer cellscell-derived xenograft mouse modelsADP-binding pocketInhibitorinhibitorinhibit

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