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].—Cancer-programmed cell death–C84H118N24O21S2—-[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.–1051366-32-5–1864.11—-O=C(N(CCC1)[C@]1([H])C(N[C@H](C(N[C@H](C(N[C@H]2C)=O)CC3=CN=CN3)=O)CC(C=C4)=CC=C4O)=O)[C@](CCC5)([H])N5C([C@@H](NC([C@@H](NC([C@@H](NC([C@@](CSSC[C@](C(N[C@H](C(N[C@H](C(N6[C@]7([H])CCC6)=O)C)=O)CO)=O)([H])NC2=O)([H])NC([C@@H](NC([C@@H](NC([C@@H](NC7=O)CCN)=O)CCCNC(N)=N)=O)CC(C=C8)=CC=C8O)=O)=O)CC(C=C9)=CC=C9O)=O)CCC(N)=O)=O)CCCCN)=O–Cancer–10 mM in DMSO–Arrestin;CXCR–CXCR4–GPCR/G Protein;Immunology/Inflammation–Peptides