Perenostobart
Based on 1 Customer Validation
Perenostobart (SRF617) is a human IgG4 antibody with inhibitory activity against CD39 ATPase. Perenostobart inhibits CD39-mediated hydrolysis of extracellular ATP to AMP, with IC50 values of 1.9 nM (HEK293 OE cells), 0.7 nM (MOLP-8 cells), and 1.2 nM (RBC-lysed whole blood). Perenostobart enhances CD4+ T-cell proliferation, promotes dendritic cell maturation, and boosts inflammasome activation in macrophages in the presence of ATP. Perenostobart demonstrates significant single-agent anti-tumor efficacy in MOLP-8 and H520 xenograft models. Perenostobart can be used for the study of cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 97.00%
- CAS. Nr.: 2643331-31-9
- Molecular Weight:145.5 kDa
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Speicherung:Shipping with dry ice
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
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
Isotype
Human IgG4 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
ENTPD1/CD39
In Vitro
Perenostobart (0.001-10 μg/mL, 1 h pretreatment) specifically binds to HEK293 cells overexpressing human CD39 (HEK293 OE), human multiple myeloma MOLP-8 cells, and primary human B cells in a dose-dependent manner[1].
Perenostobart (0.001-10 μg/mL, 1 h pretreatment) concentration-dependently inhibits CD39 ATPase activity in HEK293 OE cells, MOLP-8 cells, and RBC-lysed whole blood, with IC50 values of 0.3 μg/mL (1.9 nM), 0.1 μg/mL (0.7 nM), and 0.2 μg/mL (1.2 nM) respectively[1].
Perenostobart (10 μg/mL, 1 h pretreatment) significantly increases CD86 expression, promotes the secretion of IL-12/IL-23p40 and IL-16 and enhances the release of IL-1β and IL-18 from monocyte-derived macrophages[1].
Perenostobart (0.0001-100 μg/mL, 72 h) dose-dependently reduces CD39 expression on CD19+ B cells in human PBMCs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Perenostobart (15-30 mg/kg, i.p., twice weekly) effectively lowers plasma adenosine levels in Ncr nu/nu mice bearing H520 xenograft tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MOLP-8 cells (1 × 107) or H520 cells were subcutaneously (s.c.) implanted into the flanks of 5-7 week-old female SCID mice or Ncr nu/nu mice[1]
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Dosage:3, 10,15, 30 mg/kg
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Administration:i.p., twice weekly for 3 weeks
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Result:Achieved tumor growth inhibition.
Reduced in situ CD39 ATPase activity in tumors.
Increased infiltration of CD45+ immune cells and F4/80+ macrophages in tumors.
Elevated the levels of macrophage chemokines (MCP-1, MIP-1α, MIP-1β) in tumor lysates.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Pyroptosis Solutions
- Intraperitoneal/Peritoneal Dissemination Xenograft
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG4 kappa
Anwendung
ELISA, FACS, Functional assay
Verified Bioactivity
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Loaded Perenostobart on AHC2 biosensor, can bind CD39 Protein, Human (sf9, His, HY-P75417) with an affinity constant of 3.546E-09 M as determined in BLI assay. -
Flow Cytometry analysis of Raji cells labelling ENTPD1/CD39 (red) with Perenostobart (anti-ENTPD1/CD39) (HY-P990068). Goat Anti-Human IgG (Alexa Fluor 488) (HY-P83776) at a dilution of 1/1000 was used as the secondary antibody. Blue-Human IgG4 kappa (HY-P99003). Black-Unlabelled control, cells without incubation with primary antibody.
Chemical Information
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CAS. Nr. 2643331-31-9
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Appearance Liquid
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Molecular Weight 145.5 kDa
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Color Colorless to light yellow
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SMILES
[Perenostobart]
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Synonyms
SRF617
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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 (260 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
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Perenostobart Related Classifications
HY-P990068 Related Classifications
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