Duligotuzumab  (Synonyms: MEHD-7945A; RG 7597)

Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research^[1][2][3].

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

Human

Duligotuzumab (0.01-25 μM; 72 h) inhibits proliferation of HER2-positive OE33, OE19, and NCI-N87 gastric cancer cell lines with IC₅₀ values of ≈0.1 to ≈0.5 μM over 72 h, but has no effect on HER2-negative MKN28 gastric cancer cells^[1].
Duligotuzumab (0.5 μM; 7 days) reduces colony formation in HER2-positive OE33, OE19, and NCI-N87 gastric cancer cell lines over 7 days^[1].
Duligotuzumab (0.5 μM; 72 h) reduces migration of HER2-positive OE33, OE19, and NCI-N87 gastric cancer cell lines over 72 h^[1].
Duligotuzumab (0.5 μM; 72 h) induces apoptosis in HER2-positive OE33, OE19, and NCI-N87 gastric cancer cell lines over 72 h, with an apoptotic rate of ≈35% in OE33 cells^[1].
Duligotuzumab (0.5 μM; 48 h) reduces phosphorylated HER2 and HER3 levels but does not alter total or phosphorylated AKT, MAPK, or total HER2 or HER3 protein levels in HER2-positive OE33 and OE19 gastric cancer cell lines^[1].
Duligotuzumab induces antibody-dependent cell-mediated cytotoxicity in EGFR-overexpressing cell lines, with activity comparable to cetuximab^[2].
Duligotuzumab binds to EGFR with a dissociation constant of 0.4 nM^[2].
Duligotuzumab enhances antiproliferative activity in cancer cells, overcomes EGFR resistance, and enhances radiation effects compared to monospecific HER antibodies, including in cetuximab-resistant cells^[3].
Duligotuzumab potently blocks EGFR and HER3 receptors and inhibits downstream HER/ErbB signaling pathways in an in vitro system^[3].

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

2065  [NCBI] & 1956  [NCBI]

P21860 & P00533

ELISA, FACS, Functional assay

Unconjugated

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

144.78 kDa

1314238-96-4

Liquid

Colorless to light yellow

[Duligotuzumab]

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.

• 
  Human IgG1 kappa

• 
  Immobilized EGFR Protein, Human can bind Duligotuzumab. The EC₅₀ for this effect is 4.244 ng/mL.
• 
  Immobilized HER3 Protein, Human can bind Duligotuzumab. The EC₅₀ for this effect is 1.423 ng/mL.
• 
  Flow Cytometry analysis of Hela cells labelling EGFR (red) with Duligotuzumab (HY-P99866). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then cells were stained with the primary antibody at 1/200 dilution for an hour at 4℃. 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 IgG1 kappa (HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).

• [1]. Laterza MM, et al. Enhanced Antitumor Effect of Trastuzumab and Duligotuzumab or Ipatasertib Combination in HER-2 Positive Gastric Cancer Cells. Cancers (Basel). 2021;13(10):2339.  [Content Brief]

  [2]. Fayette J, et al. Randomized Phase II Study of Duligotuzumab (MEHD7945A) vs. Cetuximab in Squamous Cell Carcinoma of the Head and Neck (MEHGAN Study). Front Oncol. 2016;6:232.  [Content Brief]

  [3]. Cole, P. DULIGOTUZUMAB. Drugs of the Future 2015, 40(3): 167-172.