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Balixafortide (POL6326) is a potent, selective, and well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM, and also acts as a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. It demonstrates anti-cancer effects[1][2], blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM, and is 1000-fold more selective for CXCR4 than a large panel of receptors, including CXCR7.
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Description | Balixafortide (POL6326) is a potent, selective, and well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM, and also acts as a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. It demonstrates anti-cancer effects[1][2], blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM, and is 1000-fold more 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]. |
Alias | POL6326 |
Molecular Weight | 1864.14 |
Formula | C84H118N24O21S2 |
Cas No. | 1051366-32-5 |
Relative Density. | 1.58 g/cm3 (Predicted) |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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