In vitro: WZB117 inhibits glucose transport in human red blood cells. Cancer cell treatment with WZB117 leads to decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. All these changes are 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.
In vivo: Daily intraperitoneal injection of WZB117 at 10mg/kg resultes in 70% reduction in tumor volume of human A549 lung cancer grafted on nude mice.
|Cell lines||Human non–small cell lung cancer (NSCLC) cell|
|Preparation method||Cells were treated with compound WZB117 for 24 or 48 hours. WZB117 (10 μmol/L) was used in the experiments unless otherwise noted.|
|Incubation time||24 or 48 h|
|Animal models||BALB/cAJcl-nu/nu mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||73 mg/mL in DMSO|
Targeting the facilitative glucose transporter GLUT1 inhibits the self-renewal and tumor-initiating capacity of cancer stem cells.
Shibuya K, et al. Oncotarget. 2015 Jan 20;6(2):651-61. PMID: 25528771.
A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
Liu Y, et al. Mol Cancer Ther. 2012 Aug;11(8):1672-82. PMID: 22689530.
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