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Balixafortide

Catalog No. TP2141L   CAS 1051366-32-5
Synonyms: POL6326

Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7.

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Balixafortide Chemical Structure
Balixafortide, CAS 1051366-32-5
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Biological Description
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Description Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7.
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)[1]. Balixafortide potently inhibits pERK / pAKT signaling in the lymphoma lines Namalwa (IC50< 200 nM) and Jurkat (IC50 < 400 nM).
In vivo Balixafortide has been optimized to exhibit favorable absorption, distribution, metabolism, and excretion (ADME) characteristics in mice, demonstrating balanced plasma protein binding and enhanced stability in both plasma and microsomes[1].
Synonyms POL6326
Molecular Weight 1864.14
Formula C84H118N24O21S2
CAS No. 1051366-32-5

Storage

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 1051366-32-5 Autophagy GPCR/G Protein Immunology/Inflammation CXCR POL-6326 POL 6326 POL6326 inhibitor inhibit

 

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