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Balixafortide TFA (1051366-32-5 free base)

Catalog No. TP2141   CAS TP2141
Synonyms: Balixafortide TFA, POL6326 TFA

Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux (IC50s < 10 nM).

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Balixafortide TFA (1051366-32-5 free base) Chemical Structure
Balixafortide TFA (1051366-32-5 free base), CAS TP2141
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux (IC50s < 10 nM).
Targets&IC50 CXCR4:10 nM
In vitro Balixafortide efficiently blocks SDF-1 dependent chemotaxis of MDA MB 231 breast cancer cells (IC50 < 20 nM), Namalwa and Jurkat cells (IC50 < 10 nM). Balixafortide potently inhibits pERK / pAKT signaling in the lymphoma lines Jurkat (IC50 < 400 nM) and Namalwa (IC50< 200 nM) [1].
In vivo Balixafortide is optimized for favorable mouse absorption, distribution, metabolism, and excretion (ADME) properties with balanced plasma protein binding, microsomal stability, and greater plasma.
Synonyms Balixafortide TFA, POL6326 TFA
Molecular Weight 1896.05
Formula C82H113N22F3O23S2
CAS No. TP2141

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Zimmermann J, et al. Anti-tumor cell activity and in vitro profile of the next generation CXCR4 antagonist Balixafortide. Ann Oncol. 2018 Oct;29 Suppl 8:viii103. 2. Karpova D, et al. Mobilization of hematopoietic stem cells with the novel CXCR4 antagonist POL6326 (balixafortide) in healthy volunteers-results of a dose escalation trial. J Transl Med. 2017 Jan 3;15(1):2.

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Keywords

Balixafortide TFA (1051366-32-5 free base) TP2141 Autophagy GPCR/G Protein Immunology/Inflammation CXCR Balixafortide TFA 1051366-32-5 free base POL6326 TFA Balixafortide TFA (1051366 32 5 free base) 1051366-32-5 Balixafortide TFA (1051366325 free base) inhibitor inhibit

 

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