Balixafortide TFA||(POL6326 TFA)-陌孚医药/Medlife

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Balixafortide TFA (Synonyms: POL6326 TFA)

目录号: PL05890

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PL05890-50mg	50mg	¥12981.82	请登录
PL05890-100mg	100mg	询价	询价
PL05890-200mg	200mg	询价	询价

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中文名称	Balixafortide TFA
英文名称	Balixafortide TFA
包装储存	Sealed storage, away from moisture and lightPowder -80°C 2 years；-20°C 1 year

产品详情

Balixafortide TFA (POL6326 TFA) 是一种有效的，选择性的，耐受性好的肽类 CXCR4 拮抗剂，其 IC₅₀ 小于 10 nM。Balixafortide TFA 对 CXCR4 的选择性比包括 CXCR7 在内的许多受体高出 1000 倍。Balixafortide TFA 以 IC₅₀ < 10 nM 阻断 β-arrestin 募集和钙通量。Balixafortide TFA 还是一种有效的造血干细胞和祖细胞 (HSPC) 动员剂，并具有抗癌作用。

生物活性

Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC 50 < 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 IC 50 s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.

性状

Solid

IC50 & Target[1][2]

CXCR4 <10 nM (IC50)

体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and lightPowder -80°C 2 years；-20°C 1 year

ClinicalTrial

SequenceShortening

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

Sequence

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

参考文献

[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.

溶解度数据	In Vitro: H₂O : 100 mg/mL (50.55 mM; Need ultrasonic)DMSO : 100 mg/mL (50.55 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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