| Cas No.: | 1051366-32-5 |
| Chemical Name: | Ala-cys-ser-ala-pro-arg-tyr-cys-tyr-gln-lys-pro-pro-tyr-his cyclic (2->9)-disulfide |
| Synonyms: | POL6326;POL-6326 |
| SMILES: | C[C@@H]1NN[C@@H](CC2NC=NC=2)C(=O)N[C@@H](CC2C=CC(O)=CC=2)C(=O)N2[C@@H](CCC2)C(=O)N2[C@H](CCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC2C=CC(O)=CC=2)C(=O)N[C@@H]2C(N[C@@H](CC3C=CC(O)=CC=3)C(C([C@H](CCCNC(N)=N)NC([C@H](CCN)NC([C@@H]3N(C([C@H](C)NC([C@H](CO)NC(=O)[C@H](CSSC2)NC1=O)=O)=O)CCC3)=O)=O)=O)=O)=O |
| Formula: | C84H118N24O21S2 |
| M.Wt: | 1864.11 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. |
| Target: | CXCR4:<10 nM (IC50) |
| In Vivo: | Balixafortide is optimized for favorable mouse absorption, distribution, metabolism and excretion (ADME) properties with balanced plasma protein binding, greater plasma and microsomal stability[1]. |
| In Vitro: | Balixafortide potently inhibits pERK / pAKT signaling in the lymphoma lines Namalwa (IC50< 200 nM) and Jurkat (IC50 < 400 nM). 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]. |
| References: | [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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