Burixafor
Based on 2 publication(s) in Google Scholar
Burixafor (TG-0054) is a potent CXCR4 antagonist with a pIC50 of 7.4. Burixafor inhibits the binding of CXCL12 to CXCR4, antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, and blocks the downstream Gαᵢ-mediated inhibitory effect on cAMP signal transduction. Burixafor mobilizes CD34+ hematopoietic stem/progenitor cells (HSPC) from the bone marrow to the peripheral blood. Burixafor can be used for research on autologous hematopoietic stem cell transplantation (ASCT).
For research use only. We do not sell to patients.
- CAS No.: 1191448-17-5
- Formula: C27H51N8O3P
- Molecular Weight:566.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Burixafor
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Biological Activity
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CXCR4 7.4 (pIC50) |
Burixafor potently displaces CXCL12 from its binding to CXCR4 on HEK293 cells stably expressing SNAP-CXCR4, with a pIC50 of 7.4[1].
Burixafor potently inhibits CXCL12-induced recruitment of miniGαᵢ to CXCR4 in transiently transfected HEK293 cells, with a pIC50 of 7.7[1].
Burixafor potently inhibits CXCL12-induced recruitment of β-arrestin2 to CXCR4 in transiently transfected HEK293 cells, with a pIC50 of 8.0[1].
Burixafor potently reverses CXCL12-mediated, CXCR4-dependent inhibition of cAMP in HEK293 cells stably expressing CXCR4, with a pIC50 of 7.9[1].
Burixafor acts as a potent inverse agonist on constitutively active CXCR4N119S mutant in transiently transfected HEK293 cells, with a pIC50 of 7.5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Burixafor decreases acute rejection incidence and suppresses cardiac allograft vasculopathy in a Mycophenolate (HY-B0421)-treated swine heart transplant model[1].
Burixafor mobilizes hematopoietic stem/progenitor cells in mice, with enhanced efficacy when co-administered with Propranolol (HY-B0573B)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1191448-17-5
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Molecular Weight 566.72
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Formula C27H51N8O3P
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SMILES
NC1=CC(N2CCN(CC2)CCP(O)(O)=O)=NC(NC[C@@H]3CC[C@H](CC3)CNCCCNC4CCCCC4)=N1
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Synonyms
TG-0054
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET. [Abstract]2024 May 4;25(9):5018. PMID: 38732237 -
Mol Pharmacol
Pharmacological characterization of a clinical candidate, TG-0054, a small molecule inverse agonist targeting CXCR4. [Abstract]2025 Apr;107(4):100015. PMID: 40156952
Purity & Documentation
References
[1]. Pan KS, et al. Pharmacological characterization of a clinical candidate, TG-0054, a small molecule inverse agonist targeting CXCR4. Mol Pharmacol. 2025;107(4):100015. [Content Brief]
[2]. Sukhtankar DD, et al. Burixafor, a CXCR4 inhibitor with a differentiated kinetics profile: results of a phase 2 study for rapid cell mobilization in multiple myeloma and lymphoma patients undergoing transplant. Ann Hematol. 2026;105(3):86. Published 2026 Feb 4. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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