BPRCX807
BPRCX 807 is a selective and potent CXCR4 (CXC chemokine receptor type 4) antagonist. BPRCX 807 inhibits CXCL12-mediated ERK and Akt phosphorylation. BPRCX 807 can significantly suppress primary tumor growth. BPRCX 807 can be used for the study of hepatocellular carcinoma.
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- CAS. Nr.: 2236595-58-5
- Formel: C31H51N9O4
- Molecular Weight:613.79
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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CXCR4 |
BPRCX 807 (1.5 h) exhibits an IC50 value of 40.4 nM against HEK293T cells[1].
BPRCX 807 shows an EC50 value of 48.1 nM in CCRF-CEM cells[1].
BPRCX 807 (10 μM, 24-72 h) significantly inhibits CXCL12-induced accelerated wound closure in HCA-1 cells[1].
BPRCX 807 (0.1-1 μM, 17.5 h) significantly reduces the number of migrating HCA-1 cells at a concentration of 1 μM[1].
BPRCX 807 (10-20 μM, 24-48 h) restrains the hypoxia-induced increases in mesenchymal marker expression and alleviates the hypoxia-induced decrease in epithelial markers in HCA-1 cells in a dose-dependent manner[1].
BPRCX 807 (5-20 μM, 24 h) significantly inhibits CXCL12-mediated ERK and Akt phosphorylation in HCA-1 and JHH-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCA-1 cells
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Concentration:10 μM
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Incubation Time:0 h, 24 h, 48 h, 72 h
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Result:Significantly inhibited CXCL12-induced accelerated wound closure in HCA-1 cells.
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Cell Line:Hypoxia-induced HCA-1 cells
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Concentration:10 μM, 20 μM
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Incubation Time:24 h, 48 h
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Result:Increased in mesenchymal marker expression (including Slug, Fibronectin, N-cadherin, Vimentin, FOXC2, Zeb1, and Zeb2).
Alleviated the hypoxia-induced decrease in epithelial markers (E-cadherin, MTA-3, CLDN3, and CLDN5).
BPRCX 807 (15 mg/kg, s.c., once daily for 14 days), when used in combination with Anti-PD-1, can recruit T cells and synergistically inhibit tumor growth in mice with HCA-1 cell allogeneic transplantation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCA-1 or JHH-7 cells were orally implanted into the livers of 7-week-old C3H/HeNCrNarl mice and 9-week-old BALB/cAnN.Cg Foxnlnu/CrlNarl mice, respectively[1].
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Dosage:15 mg/kg
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Administration:S.c., once daily for 14 days
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Result:Significantly inhibited tumor growth when used alone.
The effect is strongest when used in combination with sorafenib.
Combined use significantly prolongs overall survival.
Reduced tumor-associated macrophage (TAM) infiltration (F4/80+ cells).
Reprogramed TAMs to the M1 phenotype (increased CD86+) and suppresses the M2 phenotype (decreased CD206+).
Increased cytotoxic CD8+ T cell infiltration.
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Animal Model:HCA-1 cells were in situ implanted into 7-week-old C3H/HeNCrNarl mice. For combined anti-PD-1 immunotherapy, mice were intraperitoneally injected with anti-mouse PD-1 antibodies 10 days after tumor implantation[1].
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Dosage:15 mg/kg
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Administration:S.c., once daily for 14 days
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Result:When used in combination with Anti-PD-1, it significantly increased the infiltration of CD4+ and CD8+ T cells within tumors.
Synergistically inhibited tumor growth (reducing it by 95%) and lung metastasis.
Chemical Information
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CAS. Nr. 2236595-58-5
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Molecular Weight 613.79
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Formel C31H51N9O4
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SMILES
O=C(CNCCC(N1CCC(CC1)NC2=NC(NCC3=NC(CCCNCCCNC4CCCCC4)=CO3)=NC(C)=C2)=O)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Ghasemi K, et al. MSX-122: Is an effective small molecule CXCR4 antagonist in cancer therapy? Int Immunopharmacol. 2022 Jul;108:108863. [Content Brief]
[2]. Yu SJ, et al. Protective Effect of CXCR4 Antagonist CX807 in a Rat Model of Hemorrhagic Stroke. Int J Mol Sci. 2020 Sep 25;21(19):7085. [Content Brief]
[3]. Song JS, et al. A highly selective and potent CXCR4 antagonist for hepatocellular carcinoma treatment. Proc Natl Acad Sci U S A. 2021 Mar 30;118(13):e2015433118. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BPRCX807 Related Classifications
HY-178205 Related Classifications
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