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).
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- CAS No.: 1191448-17-5
- Formule: C27H51N8O3P
- Masse moléculaire:566.72
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Activité biologique
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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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1191448-17-5
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Masse moléculaire 566.72
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
Pureté et documentation
Références
[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)
Burixafor Related Classifications
HY-19867 Related Classifications
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