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.
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- Pureté: 97.00%
- CAS No.: 2643331-31-9
- Masse moléculaire:145.5 kDa
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Human IgG4 kappa
Human
ENTPD1/CD39
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG4 kappa
ELISA, FACS, Functional assay
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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 No. 2643331-31-9
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Appearance Liquid
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Masse moléculaire 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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Livraison
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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Fiche technique (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)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)