Tepoditamab  (Synonyms: MCLA 117)

Tepoditamab (MCLA-117) is a full-length human IgG1 bispecific monoclonal antibody that binds to CLEC12A of myeloid cells and CD3 of cytotoxic T cells. Among others, CLEC12A is a myeloid differentiation antigen. Tepoditamab kills AML leukaemia mother cells and AML leukaemia stem cells, induces T cell-mediated proliferative lysis of AML cells. Tepoditamab induces upto 30-fold T-cell expansion. Tepoditamab results in moderate to strong cytokine (IFNγ, IL-6, IL-8, IL-10, and TNFα) and IFNγ release in human whole blood and PBMC, respectively. Tepoditamab can be used in acute myeloid leukaemia (AML) research^[1][2][3].

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

CLEC12A & CD3E

Tepoditamab binds specifically to CLEC12A^POS and CD3^POS cells within the normal haematopoietic compartment^[2].
Tepoditamab (1,000 ng/mL, 24-48 h) induces upregulation of CD69 and CD25 on CD4 and CD8 T cells after 24 and 48 h in HL60 cells concentration-dependently^[2].
Tepoditamab (0.1 ng/mL-10 μg/mL, 48 h) induces a concentration-dependent T cell-mediated lysis of HL60 cells at 100 ng/mL and above, as well as a mean EC₅₀ of 68 ng/mL^[2].

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

Tepoditamab has a normal FcRn-mediated half-life of 9-10 days in murine model^[2].

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

160364  [NCBI] & 916  [NCBI]

Q5QGZ9 & P07766

ELISA, FACS, Functional assay

Unconjugated

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

144.787 kDa

2044679-53-8

Liquid

Colorless to light yellow

[Tepoditamab]

Shipping with dry ice.

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

• 
  Human IgG1 kappa

• 
  Loaded Tepoditamab on AHC2 biosensor, can bind CLEC12A/MICL Protein, Human (Biotinylated, HEK293, His-Avi, HY-P77633) with an affinity constant of 1.185E-08 M as determined in BLI assay.
• 
  Immobilized CD3 epsilon Protein, Human (HEK293, His, HY-P70506) can bind Tepoditamab. The EC₅₀ for this effect is 74.47 ng/mL.
• 
  Immobilized CLEC12A/MICL Protein, Human (HEK293, Fc, HY-P77631) can bind Tepoditamab. The EC₅₀ for this effect is 67.71 ng/mL.

• [1]. Naval Daver, et al. T-cell-based immunotherapy of acute myeloid leukemia: current concepts and future developments. Leukemia. 2021 Jul;35(7):1843-1863.  [Content Brief]

  [2]. van Loo, P. F., et al., (2019). MCLA-117, a CLEC12AxCD3 bispecific antibody targeting a leukaemic stem cell antigen, induces T cell-mediated AML blast lysis. Expert opinion on biological therapy, 19(7), 721–733.  [Content Brief]

  [3]. Pieter Fokko Van Loo, et al., Preclinical Evaluation of MCLA117, a CLEC12AxCD3 Bispecific Antibody Efficiently Targeting a Novel Leukemic Stem Cell Associated Antigen in AML, Blood, Volume 126, Issue 23, 2015.