Cinrebafusp alfa  (Synonyms: PRS 343)

Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (K_d=0.3 nM) and human monomeric CD137 (4-1BB; K_d=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research^[1][2].

Human IgG4 kappa

Human IgG4 (S228P) kappa, Isotype Control

Fusion Protein

Cinrebafusp alfa (PRS 343) 结合表达 HER2 的 MCF-7 细胞和转染人 4-1BB 的 CHO 细胞，在 FACS 测定中 EC₅₀ 分别为 7.4 nmol/L，6.2 nmol/L^{[1 ]}。

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

Cinrebafusp alfa (PRS 343; 0.2-10 mg/kg; 静脉给药; 每周一次; 持续 20 天) 在移植有 HER2 阳性 SK-OV-3 肿瘤细胞的人源化小鼠模型中导致肿瘤生长抑制并且肿瘤浸润淋巴细胞呈剂量依赖性增加^[1]。
Cinrebafusp alfa (10 mg/kg; 静脉给药; 单剂量) 在雄性 CD-1 小鼠中的终末消除半衰期为 >14 天。Cinrebafusp alfa (3 mg/kg; 静脉注射; 单剂量) 在雄性食蟹猴中的终末消除半衰期约为 4 天^[1]。

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

2218515-90-1

液体

Colorless to light yellow

Shipping with dry ice.

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

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  Human IgG4 kappa

• 
  Immobilized Cinrebafusp alfa can bind Human 4-1BB/CD137 Protein (ECD, His Tag). The EC₅₀ for this effect is 1.33 ng/mL.
• 
  Immobilized Cinrebafusp alfa can bind Human Her2/ERBB2 Protein (ECD, His Tag). The EC₅₀ for this effect is 1.66 ng/mL.

• [1]. Marlon J Hinner, et al. Tumor-Localized Costimulatory T-Cell Engagement by the 4-1BB/HER2 Bispecific Antibody-Anticalin Fusion PRS-343. Clin Cancer Res. 2019 Oct 1;25(19):5878-5889.  [Content Brief]

  [2]. G. Ku, et al. 525O A phase I dose escalation study of PRS-343, a HER2/4-1BB bispecific molecule, in patients with HER2-positive malignancies. ABSTRACT ONLY, VOLUME 31, SUPPLEMENT 4, S462-S463, SEPTEMBER 01, 2020.