Perenostobart  (Synonyms: SRF617)

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^[1].

Human IgG4 kappa

Human IgG4 (S228P) kappa, Isotype Control

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 (3-30 mg/kg, i.p., twice weekly for 3 weeks) exhibits significant anti-tumor efficacy against MOLP-8 xenograft tumors in 5-7 week-old female SCID mice^[1].
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.

953  [NCBI]

P49961

ELISA, FACS, Functional assay

Unconjugated

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

145.5 kDa

2643331-31-9

Liquid

Colorless to light yellow

[Perenostobart]

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG4 kappa

• 
  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.

• [1]. Warren MC, et al. SRF617 Is a Potent Inhibitor of CD39 with Immunomodulatory and Antitumor Properties. Immunohorizons. 2023 May 1;7(5):366-379.  [Content Brief]