| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PGK1[1]
PGK1 (phosphoglycerate kinase 1), targeting the ADP-binding pocket with Kd = 20.9 microM for human PGK1. |
|---|---|
| ln Vitro |
Z57346765 reduces the metabolic enzyme activity of PGK1 during glycolysis and inhibits PGK1-dependent cell proliferation. It regulates lipid peroxidation and cancer cell growth, and promotes lipid peroxidation in cervical cancer cells. The compound induces expression changes in genes involved in cellular metabolism, DNA replication, and cell cycle progression. Z57346765 has been identified as a novel PGK1 inhibitor with potent anti-KIRC effects by suppressing PGK1 metabolic enzyme activity in glycolysis.
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| ln Vivo |
Z57346765 exhibits effective antitumor activity against kidney renal clear cell carcinoma (KIRC) in vivo. The compound inhibits PGK1-dependent cancer cell proliferation and has been shown to suppress tumor growth in preclinical cancer models. Z57346765 also promotes lipid peroxidation and regulates cellular metabolism, contributing to its anticancer effects. It is a valuable tool for studying the role of PGK1 in tumor metabolism, especially in renal clear cell carcinoma.
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| Enzyme Assay |
The binding affinity of Z57346765 to human PGK1 was determined with a Kd of 20.9 microM, targeting the ADP-binding pocket of the enzyme. Enzyme activity assays measuring PGK1 metabolic enzyme activity in glycolysis were used to evaluate the inhibitory effects. Screening of novel PGK1 inhibitors was performed to identify compounds with potent anti-KIRC effects by suppressing PGK1 activity. Binding studies confirmed the specificity of Z57346765 for PGK1 and its interaction with the ADP-binding site.
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| Cell Assay |
Cell proliferation assays were performed using kidney renal clear cell carcinoma cell lines, including KIRC cells, treated with Z57346765. Metabolic enzyme activity of PGK1 was measured in cell lysates following treatment to assess inhibition of glycolysis. Gene expression changes related to metabolism, DNA replication, and cell cycle were analyzed using standard molecular biology techniques. Lipid peroxidation levels were quantified in cervical cancer cells to evaluate the compound's effects on cellular oxidative status.
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| Animal Protocol |
Preclinical xenograft models of kidney renal clear cell carcinoma were used to evaluate the in vivo antitumor efficacy of Z57346765. Tumor-bearing mice were treated with the compound, and tumor growth inhibition was monitored over time. The study demonstrated that Z57346765 suppresses PGK1 metabolic enzyme activity in vivo, leading to reduced tumor progression. Additional pharmacokinetic and toxicity studies in animal models may be required for further preclinical development.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Z57346765 is limited in public resources. The compound has a molecular weight of 294.35 and is highly soluble in DMSO (≥100 mg/mL). For in vivo administration, formulation using DMSO:PEG300:Tween 80:Saline (10:40:5:45) can achieve a concentration of ≥2.5 mg/mL (8.49 mM). A typical working solution preparation involves adding 100 microL of 25.0 mg/mL DMSO stock to 400 microL PEG300, then adding 50 microL Tween-80, followed by 450 microL saline. Storage requires powder storage at -20degC (3 years) and in-solvent storage at -80degC (6 months).
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| Toxicity/Toxicokinetics |
Specific toxicology data for Z57346765 is not publicly available. As a research-use only compound, standard chemical safety procedures should be followed when handling. The compound has not been evaluated for human toxicity and is not intended for clinical use. Recommended storage conditions maintain stability for prolonged periods, and appropriate personal protective equipment should be used during handling. Further toxicological assessment would be required for any translational research applications.
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| References | |
| Additional Infomation |
Z57346765 is a novel PGK1-specific inhibitor with potential applications in cancer research, particularly for kidney renal clear cell carcinoma (KIRC). Along with CHR-6494, it represents one of the first identified small-molecule inhibitors targeting PGK1 metabolic enzyme activity in glycolysis. The compound has been studied in both in vitro and in vivo models of renal cancer. Its mechanism involves inhibition of PGK1-dependent cell proliferation and induction of changes in metabolic gene expression. Z57346765 has not entered clinical trials and remains exclusively a preclinical research tool for cancer metabolism studies.
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| Molecular Formula |
C17H18N4O
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|---|---|
| Molecular Weight |
294.35
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| CAS # |
1016340-64-9
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| Appearance |
Solid powder ; Off-white to light yellow
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~339.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.49 mM) (saturation unknown) in (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.49 mM)(saturation unknown) in 10% DMSO 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD in saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3973 mL | 16.9866 mL | 33.9732 mL | |
| 5 mM | 0.6795 mL | 3.3973 mL | 6.7946 mL | |
| 10 mM | 0.3397 mL | 1.6987 mL | 3.3973 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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