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].

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.

1978.16

C₈₆H₁₁₉F₃N₂₄O₂₃S₂

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

Cyclo(ACSAP-{Dab}-RYCYQKPPYH)(Disulfide bridge: Cys2-Cys9)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)

H₂O : 100 mg/mL (50.55 mM; Need ultrasonic)

DMSO : 100 mg/mL (50.55 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

  Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.26 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.26 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (1.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.