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BPRCX807

Chemical Structure : BPRCX807

CAS No.: 2236595-58-5

BPRCX807 (BPRCX-807)

Catalog No.: PC-49200Not For Human Use, Lab Use Only.

BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.
BPRCX807 is a clean and specific CXCR4 antagonist, shows no significant activity against other chemokine receptors including 10 CCRs, 7 CXCRs, and 1 CX3CR subtypes.
BPRCX807 can effectively inhibit CXCL12/CXCR4 axis-mediated migration of HCC cells, reverses the hypoxia-induced EMT in vitro, also alleviates a hypoxia-induced decrease in the epithelial markers (E-cadherin, MTA-3, CLDN3, and CLDN5) in HCA-1 cells.
BPRCX807 suppresses metastatic progression of hepatocellular carcinoma (HCC), and sensitizes HCC to sorafenib treatment in orthotopic HCC models, inhibits angiogenesis and remodels the immunosuppressive tumor microenvironment in the orthotopic HCA-1 model.
BPRCX807 demonstrated synergistic effects with immune therapy anti-PD-1 Ab in the orthotopic HCA-1 model.

Physicochemical Properties

M.Wt 613.808
Formula C31H51N9O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(3-(4-((2-(((4-(3-((3-(cyclohexylamino)propyl)amino)propyl)oxazol-2-yl)methyl)amino)-6-methylpyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropyl)glycine

References

1. Jen-Shin Song, et al. Proc Natl Acad Sci U S A. 2021 Mar 30;118(13):e2015433118.

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