Flotetuzumab (MGD006; S80880) 是一种双特异性CD123/CD3双亲和再靶向 (DART) 抗体。Flotetuzumab 通过同时结合靶细胞的CD123和效应 T 细胞的CD3，而重新激活 T 细胞，导致 T 细胞介导的靶细胞的细胞毒性。Flotetuzumab 对小鼠中急性髓系白血病 (AML) 患者来源异种移植物 (PDX) 模型具有抑制效力。
| 生物活性 | Flotetuzumab (MGD006; S80880) is an investigationalCD123/CD3bispecificdual-affinity retargeting antibody(DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding toCD123in target cells andCD3in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML)[1][2]. |
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体外研究
(In Vitro) | Flotetuzumab (0.01 ng/mL, 0.1 ng/mL; 144 h) 增加原发性 PBMC 细胞 中 IFN-γ、IL-10 和 IL-6 的分泌[1]。
Flotetuzumab (10-6-102ng/mL; 24 h) 在人或食蟹猴的 PBMC 细胞 (Kasumi-3 AML细胞系) 具有细胞毒性[1]。
Flotetuzumab (0.01 ng/mL, 0.1 ng/mL; 6 d) 剂量依赖性地抑制白血病母细胞生长[1]。
Cell Viability Assay[1] | Cell Line: | Primary PBMCs | | Concentration: | 0.01 ng/mL, 0.1 ng/mL | | Incubation Time: | 6 days | | Result: | Resulted in a dose-dependent depletion of leukemic blasts, accompanied by a concomitant expansion of autologous T cells, up-regulation of the proliferation marker Ki-67, and a proportionally greater expansion of CD8+cells. |
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体内研究
(In Vivo) | Flotetuzumab (0.5-4 μg/kg; 腹腔内注入; 连续输注 6 天) 在人外周血单个核细胞 (PBMC) 重建荷瘤小鼠中显示抗肿瘤活性[1]。
Flotetuzumab (0.5 mg/kg; 每 5 天 1 次; 共 30 天) 提高小鼠 NTPL-146 患者源性异种移植 (PDX) 急性髓系白血病 (AML) 模型小鼠存活率并诱导 T 细胞增殖[2]。
| Animal Model: | PBMCs-reconstituted tumor model: NSG/β2m-/-mice intradermally implanted with the KG-1a (AML-M0) cells on day 0 and intraperitoneally injected with human PBMCs on day 1[1] | | Dosage: | 0.5 μg/kg, 1 μg/kg, and 4 μg/kg; | | Administration: | Peritoneally implantation with mini-osmotic pumps; continuous infusion from days 16 to 22; | | Result: | Inhibited tumor volume significantly. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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