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Motixafortide (BL-8040, BKT140) CXCR4 Antagonist

Cat.No.S9665

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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Quality Control

Batch: Purity: 99.36%
99.36

Solubility

In vitro
Batch:

Water : 100 mg/mL

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Chemical Information, Storage & Stability

Molecular Weight 2159.52 Formula

C97H144FN33O19S2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 664334-36-5 -- Storage of Stock Solutions

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(=N)N)CC7=CC=C(C=C7)O

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Mechanism of Action

Targets/IC50/Ki
ERK
Bcl-2
MCL-1
cyclin-D1
CXCR4
(Cell-free assay)
1 nM
In vitro

Treatment with Motixafortide (BL-8040) induces the robust mobilization of AML blasts from the BM. In addition, AML cells exposed to this compound undergo differentiation. It also 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.

In vivo

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

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-05)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06506461 RECRUITING
Sickle Cell Disease
St. Jude Children's Research Hospital
2025-03-21 PHASE1
NCT07392970 RECRUITING
Acute Myeloid Leukemia; Measurable Residual Disease
Washington University School of Medicine
2026-07-23 PHASE2
NCT04543071 RECRUITING
Pancreatic Cancer; Adenocarcinoma of the Pancreas; Adenocarcinoma
Gulam Manji
2020-11-09 PHASE2
NCT06442761 RECRUITING
Sickle Cell Disease
St. Jude Children's Research Hospital
2024-11-14 PHASE1
NCT06514508 RECRUITING
Multiple Myeloma
Guangzhou Gloria Biosciences Co., Ltd.
2025-12-01 PHASE3
NCT07101445 RECRUITING
Multiple Myeloma
Emory University
2025-09-24 PHASE4

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