1. GPCR/G Protein Protein Tyrosine Kinase/RTK Immunology/Inflammation
  2. CXCR VEGFR
  3. Burixafor hydrobromide

Burixafor hydrobromide  (Synonyms: TG-0054 hydrobromide)

Cat. No.: HY-19867A Purity: ≥98.0%
Handling Instructions Technical Support

Burixafor (TG-0054) hydrobromide is a selective, orally active CXCR4 antagonist that effectively blocks the interaction between CXCR4 and its ligand, stromal cell-derived factor SDF-1. Burixafor hydrobromide interferes with the SDF-1/CXCR4 signaling pathway, prompting the release of bone marrow stem cells into the peripheral circulation, exerting immunomodulatory and anti-inflammatory activities. Burixafor hydrobromide can be used in the study of cancer, Intraocular neovascular diseases (such as choroidal neovascularization), myocardial infarction and other diseases, with the potential to mobilize stem cells, improve cardiac function and reduce inflammatory responses.

For research use only. We do not sell to patients.

Burixafor hydrobromide Chemical Structure

Burixafor hydrobromide Chemical Structure

CAS No. : 1191450-19-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

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2 Publications Citing Use of MCE Burixafor hydrobromide

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  • Customer Review

Description

Burixafor (TG-0054) hydrobromide is a selective, orally active CXCR4 antagonist that effectively blocks the interaction between CXCR4 and its ligand, stromal cell-derived factor SDF-1. Burixafor hydrobromide interferes with the SDF-1/CXCR4 signaling pathway, prompting the release of bone marrow stem cells into the peripheral circulation, exerting immunomodulatory and anti-inflammatory activities. Burixafor hydrobromide can be used in the study of cancer, Intraocular neovascular diseases (such as choroidal neovascularization), myocardial infarction and other diseases, with the potential to mobilize stem cells, improve cardiac function and reduce inflammatory responses[1][2][3].

IC50 & Target[1]

CXCR4

 

In Vitro

Burixafor hydrobromide (1 μM; 2 h) inhibits microenvironment-induced phosphorylation of Pyk2 (Y579/Y580) and FAK (Y925) in human glioblastoma (GBM) cell lines and suppresses cell migration and invasion[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Primary human glioblastoma cell lines (CL1, CL2, CL3)
Concentration: 1 μM
Incubation Time: 120 min
Result: Significantly reduced the phosphorylation of Pyk2 (Y579/Y580) and FAK (Y925) induced by microglia-conditioned medium (MCM) in all three GBM cell lines, with reductions ranging from 30-50% compared to untreated controls.
In Vivo

Burixafor hydrobromide (2.85 mg/kg; intravenous injection; 2 times) mobilizes CD34+CXCR4+, CD133+CXCR4+, and CD271+CXCR4+ cells into the peripheral circulation in the Taiwan Blue Island miniature pig myocardial infarction model, reduces the levels of TNF-α, IL-1β, and IL-6 in the myocardium and plasma, and improves left ventricular ejection fraction (LVEF)[2].
Burixafor hydrobromide (1.5 mg/50 μL; intravitreal injection; single dose) achieves sustained delivery to the retina and choroid via polylactic acid (PLA) microparticles in the New Zealand white rabbit choroidal neovascular disease model, exerting anti-angiogenic activity[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Taiwanese Lanyu miniature pigs (4-6 months old, 25-40 kg) with myocardial infarction induced by balloon occlusion of the left anterior descending coronary artery[2]
Dosage: 2.85 mg/kg
Administration: Intravenous injection, twice at 3 days and 7 days post-myocardial infarction.
Result: Increased peripheral blood white blood cell counts and CXCR4+ cells, mobilized hematopoietic and mesenchymal stem cells, reduced myocardial and plasma levels of TNF-α, IL-1β, and IL-6, and preserved left ventricular ejection fraction at 12 weeks post-myocardial infarction compared to saline controls.
Clinical Trial
Molecular Weight

769.01

Formula

C27H51N8O3P.5/2HBr

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (65.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3004 mL 6.5019 mL 13.0037 mL
5 mM 0.2601 mL 1.3004 mL 2.6007 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 20 mg/mL (26.01 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.3004 mL 6.5019 mL 13.0037 mL 32.5093 mL
5 mM 0.2601 mL 1.3004 mL 2.6007 mL 6.5019 mL
10 mM 0.1300 mL 0.6502 mL 1.3004 mL 3.2509 mL
15 mM 0.0867 mL 0.4335 mL 0.8669 mL 2.1673 mL
20 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6255 mL
25 mM 0.0520 mL 0.2601 mL 0.5201 mL 1.3004 mL
30 mM 0.0433 mL 0.2167 mL 0.4335 mL 1.0836 mL
40 mM 0.0325 mL 0.1625 mL 0.3251 mL 0.8127 mL
50 mM 0.0260 mL 0.1300 mL 0.2601 mL 0.6502 mL
60 mM 0.0217 mL 0.1084 mL 0.2167 mL 0.5418 mL

* 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.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Burixafor hydrobromide
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