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Motixafortide (BL-8040)

Name: Motixafortide (BL-8040)
Brand: Selleck Chemicals
SKU: S9665

Synonyms: BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140

Catalog No.S9665 Purity: 99.36%

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.

Motixafortide (BL-8040) Chemical Structure

CAS: 664334-36-5

Purity & Quality Control

Batch: Purity: 99.36%

99.36

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Biological Activity

Description

Targets

ERK ^[1]	Bcl-2 ^[1]	MCL-1 ^[1]	cyclin-D1 ^[1]	CXCR4 ^[1] (Cell-free assay)
				1 nM

In vitro
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]
Cell Research	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.

In Vivo
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]
Animal Research	Animal Models	female NOD scid gamma (NSG) mice (7-9 weeks old)
	Dosages	400 μg/mouse
	Administration	SC

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02115672	Withdrawn	Chronic Myeloid Leukemia	Sheba Medical Center	November 2014	Phase 1\|Phase 2

References

[1] M Abraham, et al. Leukemia. 2017 Nov;31(11):2336-2346.

Chemical lnformation & Solubility

Molecular Weight	2159.52	Formula	C₉₇H₁₄₄FN₃₃O₁₉S₂
CAS No.	664334-36-5	SDF	--
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(=N)N)CC7=CC=C(C=C7)O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

Water : 100 mg/mL

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In vivo
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