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LY2510924 is a potent and selective CXCR4 antagonist, which blocks SDF-1 binding to CXCR4 with IC50 of 0.079 nM. LY2510924 inhibits SDF-1-induced cell migration (IC50 = 0.26 nM) in human lymphoma U937 cells expressing endogenous CXCR4. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.
| Cell Experiment | |
|---|---|
| Cell lines | U937 cells |
| Preparation method | Briefly, U937 cells were harvested and washed once with chemotaxis assay buffer prepared with 1× RPMI medium containing 10 mmol/L HEPES, pH 7.5, and 0.3% BSA. Cells were then resuspended in assay buffer at a density of 5 × 106 cells/mL. The assay was performed in a 96-well ChemoTx plate (NeuroProbe). Generally, 50 μL of cell mixture with or without LY2510924 was plated on the upper chamber, and 30 μL of SDF-1α (10 ng/mL) prepared in 1× chemotaxis buffer was added to the lower chamber. The plate was then incubated for 2.5 hours at 37°C. Following the incubation, 5 μL of CellTiter 96 AQ (Promega) was added into the lower chamber. The plate was then incubated for 60 minutes at 37°C. The migrated cells were detected by measuring the absorbance at 492 nm with a Tecan Spectrafluor Plus Microplate Reader. |
| Concentrations | 0-10 uM |
| Incubation time | 2.5 h |
| Animal Experiment | |
|---|---|
| Animal models | female C57/BL6 mice, male Sprague-Dawley rats, male Beagle dogs, and male Cynomolgus monkeys at fasted state |
| Formulation | formulated in 1× PBS |
| Dosages | 3 mg/kg |
| Administration | s.c. or i.v. |
| Molecular Weight | 1189.45 |
| Formula | C62H88N14O10 |
| CAS Number | 1088715-84-7 |
| Solubility (25°C) | Water 45 mg/mL DMSO 120 mg/mL |
| Storage | -20°C, sealed |
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