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Balixafortide TFA

CAS No. :

MCE 国际站：Balixafortide TFA

产品活性：Balixafortide TFA (POL6326 TFA) 是一种选择性的，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 还是一种造血干细胞和祖细胞 (HSPC) 动员剂，并具有抗癌作用。

研究领域：GPCR/G Protein | Immunology/Inflammation

作用靶点：CXCR

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).

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.

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