Burixafor hydrobromide  (Synonyms: TG-0054 hydrobromide)

Burixafor (TG-0054) hydrobromide is a potent CXCR4 antagonist with a pIC₅₀ of 7.4. Burixafor hydrobromide 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 hydrobromide mobilizes CD34⁺ hematopoietic stem/progenitor cells (HSPC) from the bone marrow to the peripheral blood. Burixafor hydrobromide can be used for research on autologous hematopoietic stem cell transplantation (ASCT)^[1][2].

Burixafor hydrobromide potently displaces CXCL12 from its binding to CXCR4 on HEK293 cells stably expressing SNAP-CXCR4, with a pIC₅₀ of 7.4^[1].
Burixafor hydrobromide potently inhibits CXCL12-induced recruitment of miniGαᵢ to CXCR4 in transiently transfected HEK293 cells, with a pIC₅₀ of 7.7^[1].
Burixafor hydrobromide potently inhibits CXCL12-induced recruitment of β-arrestin2 to CXCR4 in transiently transfected HEK293 cells, with a pIC₅₀ of 8.0^[1].
Burixafor hydrobromide potently reverses CXCL12-mediated, CXCR4-dependent inhibition of cAMP in HEK293 cells stably expressing CXCR4, with a pIC₅₀ of 7.9^[1].
Burixafor hydrobromide 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 hydrobromide mobilizes mesenchymal stem cells, reduces inflammation, and maintains cardiac systolic function in a porcine myocardial infarction model^[1].
Burixafor hydrobromide decreases acute rejection incidence and suppresses cardiac allograft vasculopathy in a Mycophenolate (HY-B0421)-treated swine heart transplant model^[1].
Burixafor hydrobromide 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.

769.01

C₂₇H₅₁N₈O₃P.5/2HBr

1191450-19-7

Solid

Light yellow to yellow

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

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [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]