WZ811 is a highly competitive CXCR4 antagonist with oral activity. WZ811 effectively inhibited CXCR4/SDF-1 (also known as CXCL12) -mediated regulation of cAMP level (EC50=1.2 nM) and SDF-1-induced matrix glue invasion (EC50=5.2 nM) in cells.
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Source | PLoS One (2017). Figure 2. WZ 811 |
| Method | Cytotoxicity assay | |
| Cell Lines | U87.CD4.CXCR4 cells | |
| Concentrations | 100 μM | |
| Incubation Time | - | |
| Results | 100 μMof CTCE-9908, WZ811 and Me6TREN did not affect the calcium flux evoked by CXCL12 (IC50s >100,000 nM) |
| Molecular Weight | 290.36 |
| Formula | C18H18N4 |
| CAS Number | 55778-02-4 |
| Solubility (25°C) | DMSO 10 mg/mL |
| 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.
[2] Zhan W, et al. J Med Chem. Discovery of small molecule CXCR4 antagonists.
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