| Bioactivity | Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM. | ||||||
| Invitro | Motixafortide (BKT140) displays selective toxicity toward AmL and MM cells. Treatment with Motixafortide (BKT140) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. Motixafortide (BKT140) specifically triggers CXCR4-dependent cell death in leukemia and MM cells. Motixafortide (BKT140) stimulates apoptotic cell death in leukemia and MM cells[2]. | ||||||
| In Vivo | Subcutaneous injections of Motixafortide (BKT140) significantly reduces, in a dose-dependent manner, the growth of human acute myeloid leukemia and multiple myeloma xenografts. Tumors from animals treated with Motixafortide (BKT140) are smaller in size and weights, had larger necrotic areas and high apoptotic scores[2]. | ||||||
| Name | Motixafortide | ||||||
| CAS | 664334-36-5 | ||||||
| Shortening | 4F-Benzoyl-RR-{2-Naph-Ala}-CY-{Cit}-KKPYR-{Cit}-CR-NH2 (Disulfide bridge: Cys4-Cys13) | ||||||
| Formula | C97H144FN33O19S2 | ||||||
| Molar Mass | 2159.52 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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| Reference | [1]. Peled A, et al. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cellsin patients with multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79. [2]. Beider K, et al. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011 Mar;39(3):282-92. |