Motixafortide (BL-8040)

For research use only.

Catalog No.S9665 Synonyms: BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140

Motixafortide (BL-8040) Chemical Structure

CAS No. 664334-36-5

Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

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Biological Activity

Description Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
Targets
ERK [1]
()
Bcl-2 [1]
()
MCL-1 [1]
()
cyclin-D1 [1]
()
CXCR4 [1]
(Cell-free assay)
1 nM
In vitro

Treatment with BL-8040 induces the robust mobilization of AML blasts from the BM. In addition, AML cells exposed to BL-8040 undergoes differentiation. 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. Overexpression of miR-15a/miR-16-1 directly induces leukemic cell death. BL-8040-induced apoptosis is also mediated by the inhibition of survival signals via the AKT/ERK pathways.[1]

In vivo

BL-8040 induces the apoptosis of AML cells in vivo. Treatment with a BCL-2 inhibitor induces apoptosis and acts together with BL-8040 to enhance cell death. BL-8040 also synergizes with FLT3 inhibitors to induce AML cell death. Importantly, this combined treatment prolongs the survival of tumor-bearing mice and reduces minimal residual disease in vivo.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: The leukemic cell lines (MV4-11, THP-1, U937, HL-60)
  • Concentrations: 0.1 μM, 1 μM, 10 μM, 20 μM
  • Incubation Time: 24 h, 48 h
  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: female NOD scid gamma (NSG) mice (7-9 weeks old)
  • Dosages: 400 μg/mouse
  • Administration: SC
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (46.3 mM)
Ethanol '-1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 2159.52
Formula

C97H144FN33O19S2

CAS No. 664334-36-5
Storage powder
in solvent
Synonyms BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140
Smiles C1CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2C1)CCCCN)CCCCN)CCCNC(=O)N)CC3=CC=C(C=C3)O)NC(=O)C(CC4=CC5=CC=CC=C5C=C4)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C6=CC=C(C=C6)F)C(=O)NC(CCCNC(=N)N)C(=O)N)CCCNC(=O)N)CCCNC(䲧瘆Ỵ瘇㧀瘅膉疴

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02763384 Recruiting Drug: BL-8040|Drug: Nelarabine T-Acute Lymphoblastic Leukemia|Adult T Lymphoblastic Lymphoma Washington University School of Medicine|The Leukemia and Lymphoma Society|National Institutes of Health (NIH)|National Cancer Institute (NCI) December 2 2016 Phase 2
NCT02115672 Withdrawn Drug: BL-8040 Chronic Myeloid Leukemia Sheba Medical Center November 2014 Phase 1|Phase 2

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CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID