| CAS | 664334-36-5 |
| Sequence | 4-Fluorobenzoyl-Arg-Arg-2-Nal-Cys-Tyr-Cit-Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys-Arg-NH2 (Disulfide bond) |
| Sequence Single | 4-Fluorobenzoyl-RR-2-Nal-CY-Cit-KkPYR-Cit-CR-NH2 |
| Molecular Formula | C97H144FN33O19S2 |
| Molecular Weight | 2159.55 |
| Synonyms | 4F-benzoyl-TN14003, BL-8040 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Cancer Research |
| Description | BKT140 also called 4F-benzoyl-TN14003, BL-8040, is a biostable, high-affinity chemokine receptor CXCR4 antagonist with an IC50 vakue of ～1 nM, which binds CXCR4 with a greater affinity than plerixafor. When combined with G-CSF (granulocyte colony-stimulating factor), BKT140 is a safe and efficient stem cell mobilizer that enabled the collection of a high number of CD34+ cells in 1 and 2 aphaeresis procedures, resulting in successful engraftment. |
| References | 1. Synthesis of non-proteinogenic phenylalanine derivatives by rhodium-catalyzed [2+2+2] cycloaddition reactions. L.Garcia et al., Org. Biomol. Chem., 7, 5020 (2009) 2. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cellsin patients with multiple myeloma. Peled A, et al. Clin Cancer Res. 2014 Jan 15;20(2):469-79. 3. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Beider K, et al. Exp Hematol. 2011 Mar;39(3):282-92. |