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。
Balixafortide Chemical Structure
CAS No. : 1051366-32-5
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Balixafortide 的其他形式现货产品:
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]. |
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IC50 Target[1] |
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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. |
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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. |
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Clinical Trial |
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分子量 |
1864.14 |
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Formula |
C84H118N24O21S2 |
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CAS 号 |
1051366-32-5 |
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Sequence |
Cyclo(Ala-Cys-Ser-Ala-Pro-{Dab}-Arg-Tyr-Cys-Tyr-Gln-Lys-Pro-Pro-Tyr-His) (Disulfide bridge: Cys2-Cys9) |
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Sequence Shortening |
Cyclo(ACSAP-{Dab}-RYCYQKPPYH) (Disulfide bridge: Cys2-Cys9) |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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