Balixafortide  (Synonyms: POL6326)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Balixafortide is optimized for favorable mouse absorption, distribution, metabolism and excretion (ADME) properties with balanced plasma protein binding, greater plasma and microsomal stability^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1864.11

C₈₄H₁₁₈N₂₄O₂₁S₂

1051366-32-5

Cyclo(Ala-Cys-Ser-Ala-{D-Pro}-{Dab}-Arg-Tyr-Cys-Tyr-Gln-Lys-{D-Pro}-Pro-Tyr-His) (Disulfide bridge: Cys2-Cys9)

Cyclo(ACSA-{D-Pro}-{Dab}-RYCYQK-{D-Pro}-PYH) (Disulfide bridge: Cys2-Cys9)

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]