Zimberelimab  (Synonyms: GLS-010; AB-122; WBP-3055)

Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC₅₀ of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC₅₀ values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma^[1][2].

Human IgG4 lambda

Human IgG4 (S228P) lambda1, Isotype Control

Human

PDCD1/PD-1/CD279

Zimberelimab has an EC₅₀ of 210 pM for human PD-1 but does not bind to related CD28 family receptors, such as ICOS, CD28 and CTLA-4^[1].
Zimberelimab binding to cell-expressed human PD-1 inhibits the interaction of the receptor with both human PD-L1 and PD-L2 with IC₅₀s of 580 pM and 670 pM, respectively^[1].
Zimberelimab dose-dependently enhances IFN-γ production and proliferation by CD4⁺ T cells, saturating at concentrations below 100 pM^[1].

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

Zimberelimab (10 and 20 mg/kg; i.v.; BIW*3) shows significant anti-tumor effects in mice^[2].
PK parameters of Zimberelimab after single vd administrations of 2, 6, and 18 mg/kg in cynomolgus macaques^[2]

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

5133  [NCBI]

Q15116

ELISA, FACS, Functional assay

Unconjugated

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

144.41 kDa

2259860-24-5

Liquid

Colorless to light yellow

[Zimberelimab]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

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

• 
  Human IgG4 lambda

• 
  Immobilized PD-1 Protein (ECD, His Tag), Human can bind Zimberelimab. The EC₅₀ for this effect is 3.01 ng/mL.
• 
  Flow cytometric analysis of 1X10⁶ 10 ng/mL PMA and 1 μg/mL Ionomycin co-stimulated Jurkat cells (24h) with Zimberelimab (HY-P99109, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 lambda1 (HY-P99987, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).

• [1]. Markham A. Zimberelimab: First Approval. Drugs. 2021 Nov;81(17):2063-2068.  [Content Brief]

  [2]. Lou B, et al. Preclinical Characterization of GLS-010 (Zimberelimab), a Novel Fully Human Anti-PD-1 Therapeutic Monoclonal Antibody for Cancer. Front Oncol. 2021 Sep 15;11:736955.  [Content Brief]