Tarextumab  (Synonyms: OMP 59R5; Anti-Human NOTCH2 Recombinant Antibody)

Tarextumab (OMP-59R5) is a cross-reactive, fully human IgG2 antibody that selectively inhibits Notch2 and Notch3 signaling. Tarextumab demonstrates broad-spectrum antitumor efficacy in xenograft models of epithelial tumors. Tarextumab can be used for the study of pancreatic cancer^[1][2].

Human IgG2 kappa

Human IgG2 kappa, Isotype Control

Human

NOTCH3

Tarextumab inhibits human Notch2 and Notch3 signaling activity (reduces RLU values) without affecting Notch1 in HeLa cells using a Notch-responsive luciferase reporter assay^[1].
Tarextumab downregulates mRNA expression of human Notch2, Notch3, HES1, NANOG, and OCT4, and reverses Gemcitabine (HY-17026)-induced upregulation of EMT-related genes (CDH2, VIM, FN1) in OMP-PN17 pancreatic tumor cells^[1].
Tarextumab reduces protein levels of Notch3 extracellular domain (ECD) and active intracellular domain (ICD) in OMP-PN17 pancreatic tumor cells, and decreases the number of cells with high Notch3 ECD staining^[1].

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

Tarextumab (40 mg/kg, i.p., every other week) combined with Gemcitabine (HY-17026) inhibits tumor growth and induces tumor regression in pancreatic cancer PDX models in NOD/SCID mice^[1].
Tarextumab (40 mg/kg, i.p., once weekly, 4 weeks) does not induce marked tumor growth inhibition in MDA-MB-468 and HCC70 TNBC cell line-derived xenograft models in BALB/c nude mice^[2].

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

4854  [NCBI]

Q9UM47

ELISA, FACS, Functional assay

Unconjugated

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

142.94 kDa

1359940-55-8

Liquid

Colorless to light yellow

[Tarextumab]

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 IgG2 kappa

• 
  Immobilized NOTCH2 Protein (His Tag), Human can bind Tarextumab. The EC₅₀ for this effect is 1.22 ng/mL.
• 
  Flow cytometric analysis of 1X10⁶ MCF-7 cells with Tarextumab (HY-P99320, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure 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 IgG2 kappa (HY-P99002, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).

• [1]. Yen WC, et al. Targeting Notch signaling with a Notch2/Notch3 antagonist (tarextumab) inhibits tumor growth and decreases tumor-initiating cell frequency. Clin Cancer Res. 2015 May 1;21(9):2084-95.  [Content Brief]

  [2]. Fu W, et al. EGFR/Notch Antagonists Enhance the Response to Inhibitors of the PI3K-Akt Pathway by Decreasing Tumor-Initiating Cell Frequency. Clin Cancer Res. 2019 May 1;25(9):2835-2847.  [Content Brief]