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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 | |
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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 | |
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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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