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Purity: ≥98%
WZB117 is a novel and potent inhibitor of Glucose Transporter 1 (GLUT1). It not only inhibited cell growth in cancer cell lines but also inhibited cancer growth in a nude mouse model. Daily intraperitoneal injection of WZB117 at 10 mg/kg resulted in a more than 70% reduction in the size of human lung cancer of A549 cell origin. Mechanism studies showed that WZB117 inhibited glucose transport in human red blood cells (RBC), which express Glut1 as their sole glucose transporter. Cancer cell treatment with WZB117 led to decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. All these changes were followed by increase in ATP-sensing enzyme AMP-activated protein kinase (AMPK) and declines in cyclin E2 as well as phosphorylated retinoblastoma, resulting in cell-cycle arrest, senescence, and necrosis. Addition of extracellular ATP rescued compound-treated cancer cells, suggesting that the reduction of intracellular ATP plays an important role in the anticancer mechanism of the molecule. Senescence induction and the essential role of ATP were reported for the first time in Glut1 inhibitor-treated cancer cells. Thus, WZB117 is a prototype for further development of anticancer therapeutics targeting Glut1-mediated glucose transport and glucose metabolism.
| ln Vitro |
WZB117 reduced glucose transport in cancer cells in a dose-dependent manner, according to the glucose uptake assay. The assay was completed in less than a minute, indicating that WZB117-induced reduction of glucose transport may be the result of a quick and direct mechanism. WZB117 reduced cancer cell proliferation with an IC50 of about 10 μM, according to an experiment for cell viability. The clonogenic experiment verified WZB117's inhibitory effect on cancer cell development and demonstrated the irreversible nature of this inhibition. WZB117 therapy had a far greater cell growth inhibitory effect on lung cancer A549 cells than it did on non-tumorigenic lung NL20 cells. MCF7 breast cancer cells and their non-tumorigenic MCF12A counterparts showed comparable outcomes. Greater suppression of cell development was reported when WZB117 was given to cancer cells cultivated under hypoxia settings as opposed to normoxic ones [1].
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| ln Vivo |
Compared to mock (PBS/DMSO)-treated tumors, compound-treated tumors had an average size reduction of almost 70% following daily intraperitoneal injection of WZB117 at a dose of 10 mg/kg body weight, according to animal studies. Most astonishingly, after treatment, 2 out of 10 tumors treated with compounds stopped growing and even vanished during the trial. Compared to mock-treated mice, WZB117-treated mice lost between 1 and 2 grams of body weight, with adipose tissue accounting for the majority of the weight loss. These findings were based on measurements and analysis of body weight. The study's conclusion revealed that while cell counts stayed within normal ranges, the compound-treated mice's lymphocyte and platelet counts differed from the vehicle-treated mice's. Use of glucose transport inhibitors raises certain concerns since treated mice may develop hyperglycemia [1].
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| References |
[1]. Liu Y, et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Mol Cancer Ther. 2012 Aug;11(8):1672-82
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| Molecular Formula |
C20H13FO6
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| Molecular Weight |
368.32
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| CAS # |
1223397-11-2
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| SMILES |
FC1=C(OC(C2=CC=CC(O)=C2)=O)C(OC(C3=CC=CC(O)=C3)=O)=CC=C1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. 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 (6.79 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 to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7150 mL | 13.5752 mL | 27.1503 mL | |
| 5 mM | 0.5430 mL | 2.7150 mL | 5.4301 mL | |
| 10 mM | 0.2715 mL | 1.3575 mL | 2.7150 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.
Small-molecule WZB117 and its inhibitory actions on glucose uptake and cancer cell growth.Mol Cancer Ther.2012 Aug;11(8):1672-82. |
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Small molecule WZB117 inhibits cancer growth in tumor-bearing nude mice.Mol Cancer Ther.2012 Aug;11(8):1672-82. |
Glycolysis studies: WZB117 treatment resulted in changes in levels of glycolytic proteins and metabolites and addition of ATP rescued WZB117-treated A549 cells.Mol Cancer Ther.2012 Aug;11(8):1672-82. |
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