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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]. |
| Synonyms | POL6326 |
| Molecular Weight | 1864.14 |
| Formula | C84H118N24O21S2 |
| Cas No. | 1051366-32-5 |
| Smiles | [H][C@]12CCCN1C(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCN)NC2=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@]2([H])C(=O)N2CCC[C@@]2([H])C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](C)C(=O)N1 |
| Relative Density. | 1.58 g/cm3 (Predicted) |
| Sequence | Cyclo(Ala-Cys-Ser-Ala-{D-Pro}-{Dab}-Arg-Tyr-Cys-Tyr-Gln-Lys-{D-Pro}-Pro-Tyr-His) (Disulfide bridge: Cys2-Cys9) |
| Sequence Short | Cyclo(ACSA-{D-Pro}-{Dab}-RYCYQK-{D-Pro}-PYH) (Disulfide bridge: Cys2-Cys9) |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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