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WZB117

Cat. No. M6156
WZB117  Structure
Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 350 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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.
Concentrations 10 μmol/L
Incubation time 24 or 48 h
Animal Experiment
Animal models BALB/cAJcl-nu/nu mice
Formulation DMSO
Dosages 3.6 mL/kg/day
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 368.31
Formula C20H13FO6
CAS Number 1223397-11-2
Purity >98%
Solubility 73 mg/mL in DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




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