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Motixafortide (BL-8040)

Cat. No. M10215
Motixafortide (BL-8040) Structure
Synonym:

BL-8040, BKT140, TF 14016

Size Price Availability Quantity
5mg USD 330.3  USD367 In stock
10mg USD 501.3  USD557 In stock
25mg USD 1005.3  USD1117 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 2159.52
Formula C97H144FN33O19S2
CAS Number 664334-36-5
Purity >99%
Solubility Water 90 mg/mL
Storage -20°C, sealed
References

The CXCR4 inhibitor BL-8040 induces the apoptosis of AML blasts by downregulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression
M Abraham, et al. Leukemia. 2017 Nov;31(11):2336-2346. PMID: 28280274.

The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cells in patients with multiple myeloma
Amnon Peled, et al. Clin Cancer Res. 2014 Jan 15;20(2):469-79. PMID: 24246358.

CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth
Katia Beider, et al. Exp Hematol. 2011 Mar;39(3):282-92. PMID: 21138752.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Motixafortide (BL-8040), BL-8040, BKT140, TF 14016 supplier, CXCR, inhibitors

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