Burixafor  (Synonyms: TG-0054)

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)^[1][2].

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 CXCR4^N119S 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 mobilizes mesenchymal stem cells, reduces inflammation, and maintains cardiac systolic function in a porcine myocardial infarction model^[1].
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.

566.72

C₂₇H₅₁N₈O₃P

1191448-17-5

NC1=CC(N2CCN(CC2)CCP(O)(O)=O)=NC(NC[C@@H]3CC[C@H](CC3)CNCCCNC4CCCCC4)=N1

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• [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]