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Balixafortide(POL6326)

  Cat. No.:  DC21522   Featured
Chemical Structure
1051366-32-5
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More than 5000 active chemicals with high quality for research!
Field of application
Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1051366-32-5
Chemical Name: Ala-cys-ser-ala-pro-arg-tyr-cys-tyr-gln-lys-pro-pro-tyr-his cyclic (2->9)-disulfide
Synonyms: POL6326;POL-6326
SMILES: C[C@@H]1NN[C@@H](CC2NC=NC=2)C(=O)N[C@@H](CC2C=CC(O)=CC=2)C(=O)N2[C@@H](CCC2)C(=O)N2[C@H](CCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC2C=CC(O)=CC=2)C(=O)N[C@@H]2C(N[C@@H](CC3C=CC(O)=CC=3)C(C([C@H](CCCNC(N)=N)NC([C@H](CCN)NC([C@@H]3N(C([C@H](C)NC([C@H](CO)NC(=O)[C@H](CSSC2)NC1=O)=O)=O)CCC3)=O)=O)=O)=O)=O
Formula: C84H118N24O21S2
M.Wt: 1864.11
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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].
Target: CXCR4:<10 nM (IC50)
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].
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].
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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