Balixafortide(Synonyms: POL6326)

Balixafortide;(Synonyms: POL6326)

Balixafortide (POL6326) 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 对 CXCR4 的选择性比包括 CXCR7 在内的许多受体高出 1000 倍。Balixafortide 以 IC50 < 10 nM 阻断 β-arrestin 募集和钙通量。Balixafortide 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。

Balixafortideamp;;(Synonyms: POL6326)

Balixafortide Chemical Structure

CAS No. : 1051366-32-5

规格 是否有货
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Balixafortide 的其他形式现货产品:

Balixafortide TFA

生物活性

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].

IC50 Target[1]

CXCR4

lt;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)[1].

MCE 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[1].

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

Clinical Trial

分子量

1864.14

Formula

C84H118N24O21S2

CAS 号

1051366-32-5

Sequence

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

Sequence Shortening

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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

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.