Tarextumab
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.83%
- CAS No.: 1359940-55-8
- Masse moléculaire:142.94 kDa
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Human IgG2 kappa
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., 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.
-
Animal Model:Human pancreatic cancer cells (from PDX models including OMP-PN4, OMP-PN8, OMP-PN17) were subcutaneously implanted into NOD/SCID mice[1]
-
Dosage:40 mg/kg combined with Gemcitabine (HY-17026)
-
Administration:i.p., every other week
-
Result:Achieved enhanced antitumor efficacy.
Showed striking tumor regression.
Reduced cancer stem cell (CSC) frequency.
Delayed tumor recurrence.
Decreased tumor cell proliferation.
Increased pericyte maturation (enhanced desmin-positive pericyte association with CD31-positive endothelial cells) and tumor vascular perfusion and reduced intratumoral hypoxia.
-
Animal Model:Triple-negative breast cancer (TNBC) cells (from cell lines including MDA-MB-468, HCC70) were subcutaneously implanted into BALB/c nude mice[2]
-
Dosage:40 mg/kg
-
Administration:i.p., once weekly, 4 weeks
-
Result:Reduced tumor-initiating cell (TIC) frequency.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
-
Human IgG2 kappa
ELISA, FACS, Functional assay
-
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).
Chemical Information
-
CAS No. 1359940-55-8
-
Appearance Liquid
-
Masse moléculaire 142.94 kDa
-
Color Colorless to light yellow
-
SMILES
[Tarextumab]
-
Synonyms
OMP 59R5; Anti-Human NOTCH2 Recombinant Antibody
-
Livraison
Shipping with dry ice.
-
Formulation
Please refer to the lot-specific COA for specific buffer information.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
-
Fiche technique (261 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Inhibitory Antibodies User Guide (603 KB)
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)