| Bioactivity | Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. | ||||||
| Invitro | 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]. | ||||||
| Name | Balixafortide TFA | ||||||
| Sequence | Cyclo(Ala-Cys-Ser-Ala-{D-Pro}-{Dab}-Arg-Tyr-Cys-Tyr-Gln-Lys-{D-Pro}-Pro-Tyr-His) (Disulfide bridge: Cys2-Cys9) | ||||||
| Shortening | Cyclo(ACSA-{D-Pro}-{Dab}-RYCYQK-{D-Pro}-PYH) (Disulfide bridge: Cys2-Cys9) | ||||||
| Formula | C86H119F3N24O23S2 | ||||||
| Molar Mass | 1978.16 | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |