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编 号:F746613
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CAS No: 1664355-28-5
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Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule.Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in 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).
体内研究:
Flotetuzumab (0.5-4 μg/kg; intraperitoneal implantation; continuous infusion for 6 d) shows antitumor activity in human peripheral blood mononuclear cells (PBMCs)-reconstituted tumor-bearing mice.Flotetuzumab (0.5 mg/kg; once every 5 d; for 30 d) improves mouse survival and induces T-cell proliferation in mouse NTPL-146 patient-derived xenograft (PDX) model of acute myeloid leukemia (AML).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
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.
体外研究:
Flotetuzumab (0.01 ng/mL, 0.1 ng/mL; 144 h) increases IFN-γ, IL-10, and IL-6 secretion in primary PBMCs.Flotetuzumab (10-6-102 ng/mL; 24 h) shows cytotoxicity against the Kasumi-3 AML cell line using human PBMCs or cynomolgus.Flotetuzumab (0.01 ng/mL, 0.1 ng/mL; 6 d) dose-dependently inhibits leukemic blasts growth.