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Motixafortide (BL-8040) is an antagonist of CXCR4 with IC50 value of 1 nM. Motixafortide (BL-8040) specifically triggers CXCR4-dependent cell death in leukemia and MM cells and it stimulates apoptotic cell death in leukemia and MM cells. Treatment with Motixafortide (BL-8040) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. BL-8040 induces the apoptosis of AML cells in vitro. This apoptosis is mediated by the up-regulation of miR-15a/miR-16-1, resulting in down-regulation of the target genes BCL-2, MCL-1 and cyclin-D1.
| Cell Experiment | |
|---|---|
| Cell lines | The leukemic cell lines (MV4-11, THP-1, U937, HL-60) |
| Preparation method | Cells are seeded in triplicate at 2×105 cells/well in a total volume of 250 μl in a 96-well plate in medium supplemented with 1% FCS RPMI medium for 24hr in the presence of BL-8040/AMD3100 (0.1, 1, 10 or 20μM) or ABT-199 (0.01, 0.1, 1 or 10μM). To test the combination of BL-8040 and ABT-199, cells are incubated for 24hr with BL-8040 (20μM) and ABT-199 (0.01, 0.1, 1 or 10μM). To test the combined effects of BL-8040 and AC220, cells are incubated for 48 hr with BL-8040 (20μM), AC220 (50nM) or a combination of the two. After incubation, cells are stained with propidium iodide (PI), and the percentage of dead cells (PI+ cells) in the culture is measured using a FACSCalibur machine. |
| Concentrations | 0.1 μM, 1 μM, 10 μM, 20 μM |
| Incubation time | 24 h, 48 h |
| Animal Experiment | |
|---|---|
| Animal models | female NOD scid gamma (NSG) mice (7-9 weeks old) |
| Formulation | - |
| Dosages | 400 μg/mouse |
| Administration | s.c. |
| Molecular Weight | 2159.52 |
| Formula | C97H144FN33O19S2 |
| CAS Number | 664334-36-5 |
| Solubility (25°C) | Water 90 mg/mL |
| Storage | -20°C, sealed |
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Plerixafor (AMD3100) is a CXCR4 chemokine receptor antagonist. |
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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
Plerixafor 8HCl (AMD3100 8HCl) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively. |
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