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 |
| 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.
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