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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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| Navarixin
Navarixin (SCH 527123) is a novel, selective CXCR2 receptor antagonist with IC50 of 3 nM. Navarixin (SCH 527123) has Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly. |
| AMD3465 hexahydrobromide (AMD3465 )
AMD3465 hexahydrobromide（AMD3465 ) is an effective CXCR4 antagonist that inhibits 12G5 mAb in SupT1 cells. The IC50 values of CXCL12AF647 and CXCR4 were 0.75 nM and 18 nM, respectively. AMD 3465 also effectively inhibited X4 HIV replication (IC50, 1-10 nM), but not R5 HIV replication. |
| Plerixafor 8HCl
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