Balixafortide

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Balixafortide

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1051366-32-5

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

POL6326

产品介绍

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。

生物活性

Balixafortide (POL6326) is a potent, selective, well-tolerated peptidicCXCR4antagonist with anIC₅₀< 10 nM. Balixafortide shows 1000-fold selective forCXCR4than a large panel of receptors includingCXCR7. Balixafortide blocksβ-arrestinrecruitment 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

<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].

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].

Clinical Trial

分子量

1864.14

Formula

C₈₄H₁₁₈N₂₄O₂₁S₂

CAS 号

1051366-32-5

Sequence

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

Sequence Shortening

Cyclo(ACSA-{D-Pro}-{Dab}-RYCYQK-{D-Pro}-PYH) (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.