Tebotelimab  (Synonyms: MGD-013)

Tebotelimab (MGD-013) is a humanized IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC₅₀s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity^[1][2][3].

[V-kappa'-VH-h-CH2-CH3_V-kappa-VH']2

Human IgG4 (S228P) kappa, Isotype Control

Human

PD-1 & LAG-3

MGD013 (0.39, 1.56, 6.25, 25 nM; 48 hours) enhances T-cell antigen receptor-driven Activation in human PBMCs. MGD013 shows enhanced staphylococcal enterotoxin B (SEB; 0.5mg/mL)-induced IFN-γ secretion compared to PD-1 + LAG-3 mAb combination^[1].

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

5133  [NCBI] & 3902  [NCBI]

Q15116 & P18627

ELISA, FACS, Functional assay

Unconjugated

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

166.7 kDa

2245725-04-4

Liquid

Colorless to light yellow

[Tebotelimab]

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-kappa'-VH-h-CH2-CH3_V-kappa-VH']2

• 
  Immobilized Tebotelimab can bind Human PD-1 Protein (ECD, His Tag). The EC₅₀ for this effect is 0.413 ng/mL.
• 
  Immobilized Tebotelimab can bind Human LAG-3 Protein (ECD, His Tag). The EC₅₀ for this effect is 0.423 ng/mL.
• 
  Flow cytometric analysis of 1×10⁶ Jurkat cells labelling LAG-3 (red) with Tebotelimab (HY-P99573). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 kappa Isotype Control (HY-P99003, blue) was used as the isotype control.

• [1]. Ross LaMotte-Mohs, et al. Abstract 3217: MGD013, a bispecific PD-1 x LAG-3 Dual-Affinity Re-Targeting (DART®) protein with T-cell immunomodulatory activity for cancer treatment. Cancer Res (2016) 76 (14_Supplement): 3217.

  [2]. Daniel Vt Catenacci, et al.MAHOGANY: margetuximab combination in HER2+ unresectable/metastatic gastric/gastroesophageal junction adenocarcinoma. Future Oncol. 2021 Apr;17(10):1155-1164.  [Content Brief]

  [3]. Yiming Wei, et al. LAG3-PD-1 Combo Overcome the Disadvantage of Drug Resistance. Front Oncol. 2022 Apr 14;12:831407.  [Content Brief]