BKT140 (4F-benzoyl-TN14003) is a 14-residue bio stable synthetic peptide[1][2] which binds CXCR4 with a greater affinity compared to plerixafor[1][2]. It has been conjugated on the surface of chitosan based polymer micelles[3], and has demonstrated both cytotoxic and cytostatic properties in proliferation assays[4]. BKT140 is also a high-affinity chemokine receptor CXCR4 antagonist, available for purchase from Bachem[5].
It has been shown to be a powerful inducer of hematopoietic stem cell mobilization[2] and can bind CXCR4 with a Kd of 0.11 μmol/L[3][4]. Subcutaneous administration of BKT140 has been shown to significantly delay the development of H460 and A549 xenografts[5].
BKT140 (4F-benzoyl-TN14003) is a highly selective and unique CXCR4 antagonist that binds to the receptor with high affinity (1nM)[1]. Pre-clinical studies in animal models have shown that BKT140 induces a robust mobilization of white blood cells (WBC) and hematopoietic stem cells (HSC)[2], as well as an extended K off-rate[3]. In patients with multiple myeloma, BKT140 has been found to be safe and effective in inducing CD34+ cell mobilization[4].
Reference
1
nih.gov
2
aacrjournals.org
3
rsc.org
4
sciencedirect.com
5
bachem.com