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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 1359940-55-8
- Molecular Weight:142.94 kDa
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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.
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Animal Model:Human pancreatic cancer cells (from PDX models including OMP-PN4, OMP-PN8, OMP-PN17) were subcutaneously implanted into NOD/SCID mice[1]
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Dosage:40 mg/kg combined with Gemcitabine (HY-17026)
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Administration:i.p., every other week
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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.
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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]
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Dosage:40 mg/kg
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Administration:i.p., once weekly, 4 weeks
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Result:Reduced tumor-initiating cell (TIC) frequency.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG2 kappa
ELISA, FACS, Functional assay
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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
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CAS. Nr. 1359940-55-8
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Appearance Liquid
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Molecular Weight 142.94 kDa
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Color Colorless to light yellow
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SMILES
[Tarextumab]
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Synonyms
OMP 59R5; Anti-Human NOTCH2 Recombinant Antibody
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Versand
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (261 KB)
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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)
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Inhibitory Antibodies User Guide (603 KB)
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Tarextumab Related Classifications
HY-P99320 Related Classifications
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