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.