BKT140 (4F-benzoyl-TN14003) is a 14-residue bio stable synthetic peptide which binds CXCR4 with a greater affinity compared to plerixafor. It has been conjugated on the surface of chitosan based polymer micelles, and has demonstrated both cytotoxic and cytostatic properties in proliferation assays. BKT140 is also a high-affinity chemokine receptor CXCR4 antagonist, available for purchase from Bachem.
It has been shown to be a powerful inducer of hematopoietic stem cell mobilization and can bind CXCR4 with a Kd of 0.11 μmol/L. Subcutaneous administration of BKT140 has been shown to significantly delay the development of H460 and A549 xenografts.
BKT140 (4F-benzoyl-TN14003) is a highly selective and unique CXCR4 antagonist that binds to the receptor with high affinity (1nM). Pre-clinical studies in animal models have shown that BKT140 induces a robust mobilization of white blood cells (WBC) and hematopoietic stem cells (HSC), as well as an extended K off-rate. In patients with multiple myeloma, BKT140 has been found to be safe and effective in inducing CD34+ cell mobilization.