Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC₅₀ vakue of ～1 nM.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

2159.52

C₉₇H₁₄₄FN₃₃O₁₉S₂

664334-36-5

4F-Benzoyl-RR-{2-Naph-Ala}-CY-{Cit}-KKPYR-{Cit}-CR-NH2 (Disulfide bridge: Cys4-Cys13)

Room temperature in continental US; may vary elsewhere.

H₂O : 100 mg/mL (46.31 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (46.31 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂：;PBS

  Solubility: 110 mg/mL (50.94 mM); Clear solution; Need ultrasonic

• [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.

Hematopoietic cancer cells are incubated with different concentrations of Motixafortide (BKT140) or AMD3100 for 24 hours. Motixafortide (BKT140) is treated with 1M hydrochloric acid (HCL) to achieve a pH of 2.7 to 3 at room temperature for 30 minutes and the pH is adjusted to 7 using concentrated NaOH. Proteinase K is added to Motixafortide (BKT140) at a final concentration of 100 mg/mL, incubated at 37°C for 1 hour, and inactivated by heat treatment (65°C for 30 minutes). After incubation, cells are stained with propidium iodide and the percent of viable PI-negative cells in culture is determined^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Mice: Severe combined immune-deficient (SCID)/beige mice (C.B-17/IcrHsd-SCID-bg) are used in the study. NB4 cells resuspended in PBS are injected subcutaneously into the flanks of the mice (200 μL per mouse containing 5×10⁶ cells). Tumor growth is monitored daily, and mice are randomized to drug-treated or control PBS-treated groups (10 mice per group) when the tumor size (width×length) reaches 0.04 cm². BKT140 is administered subcutaneously at a dose of 200 μg per mouse each day for 5 days^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.