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 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. |
| Molecular Weight | 368.31 |
| Formula | C20H13FO6 |
| CAS Number | 1223397-11-2 |
| Solubility (25°C) | 63 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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| SLC26A3-IN-3
SLC26A3-IN-3 is a SLC26A3 inhibitor (IC50: 40 nM). |
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