Flotetuzumab  (Synonyms: MGD006; S80880)

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)^[1][2].

V-Lambda-VH_V-Kappa-VH'

Human

CD123 & CD3

Flotetuzumab (0.01 ng/mL, 0.1 ng/mL; 144 h) increases IFN-γ, IL-10, and IL-6 secretion in primary PBMCs^[1].
Flotetuzumab (10^-6-10² ng/mL; 24 h) shows cytotoxicity against the Kasumi-3 AML cell line using human PBMCs or cynomolgus^[1].
Flotetuzumab (0.01 ng/mL, 0.1 ng/mL; 6 d) dose-dependently inhibits leukemic blasts growth^[1].

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

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^[1].
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)^[2].

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

916  [NCBI] & 3563  [NCBI]

P07766 & P26951

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

58.77 kDa

1664355-28-5

Liquid

Colorless to light yellow

[Flotetuzumab]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  V-Lambda-VH_V-Kappa-VH'

• 
  Immobilized Flotetuzumab can bind Human IL-3R alpha/CD123 Protein (hFc Tag). The EC₅₀ for this effect is 3.75 ng/mL.
• 
  Immobilized Flotetuzumab can bind Human CD3 epsilon/CD3e Protein (ECD, hFc Tag). The EC₅₀ for this effect is 1.33 ng/mL.

• [1]. Chichili GR, et al. A CD3xCD123 bispecific DART for redirecting host T cells to myelogenous leukemia: preclinical activity and safety in nonhuman primates. Sci Transl Med. 2015 May 27;7(289):289ra82.  [Content Brief]

  [2]. Barwe SP, et al. Efficacy of Flotetuzumab in Combination with Cytarabine in Patient-Derived Xenograft Models of Pediatric Acute Myeloid Leukemia. J Clin Med. 2022 Feb 28;11(5):1333.  [Content Brief]