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 预处理) 以剂量依赖方式特异性结合到过表达人 CD39 的 HEK293 细胞 (HEK293 OE)、人多发性骨髓瘤 MOLP-8 细胞和原代人 B 细胞^[1]。
Perenostobart (0.001-10 μg/mL, 1 h 预处理) 以浓度依赖方式抑制 HEK293 OE 细胞、MOLP-8 细胞和红细胞裂解全血中的 CD39 ATPase 活性，其 IC₅₀ 值分别为 0.3 μg/mL (1.9 nM)、0.1 μg/mL (0.7 nM) 和 0.2 μg/mL (1.2 nM)^[1]。
Perenostobart (10 μg/mL, 1 h 预处理) 显著增加 CD86 表达，促进单核细胞来源巨噬细胞分泌 IL-12/IL-23p40 和 IL-16，并增强 IL-1β 和 IL-18 的释放^[1]。
Perenostobart (0.0001-100 μg/mL, 72 h) 以剂量依赖方式减少人 PBMC 中 CD19⁺ B 细胞上的 CD39 表达^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Perenostobart (3-30 mg/kg, 腹腔注射, 每周两次, 持续 3 周) 在 5-7 周龄雌性 SCID 小鼠中对 MOLP-8 异种移植瘤显示出显著的抗肿瘤疗效^[1]。
Perenostobart (15-30 mg/kg, 腹腔注射, 每周两次) 在携带 H520 异种移植瘤的 Ncr nu/nu 小鼠中有效降低血浆腺苷水平^[1]。

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

液体

Colorless to light yellow

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]