MCE products for research use only. We do not sell to patients.

Zimberelimab

MCE China：Zimberelimab

Brand：MedChemExpress (MCE)

Cat. No.HY-P99109

CAS：2259860-24-5

Synonyms：GLS-010; AB-122; WBP-3055

Purity：99.90%

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

Shipping：Shipping with dry ice.

Description：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.

In Vitro：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].

In Vivo：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] PK parameters 2 mg/kg 6 mg/kg 18 mg/kg C0 (mg/mL) 103 ± 23.7 (23.0%) 157 ± 18.7 (11.9%) 508 ± 48.0 (9.46%) T1/2 (h) 111 ± 23.7 (30.5%) 115 ± 32.8 (28.5%) 129 ± 17.0 (13.1%) Vss (mL/kg) 48.4 ± 7.48 (15.5%) 49.4 ± 6.49 (13.1%) 46.3 ± 5.49 (11.8%) Cl (mL/h/kg) 0.288 ± 0.0373 (13.0%) 0.278 ± 0.0308 (11.1%) 0.183 ± 0.0293 (16.0%) Tlast (h) 396 ± 141 (35.5%) 704 ± 203 (28.9%) 816 ± 0.00 AUC0-last (h*mg/mL) 6300 ± 1320 (21.0%) 21300 ± 2570 (12.1%) 98100 ± 16300 (16.6%) AUCo?inf (h*mg/mL) 7060 ± 1020 (14.5%) 21800 ± 2310 (10.6%) 101000 ± 16700 (16.6%) MRT0-last (h) 126 ± 23.3 (18.4%) 164 ± 31.2 (19.0%) 236 ± 14.8 (6.27%) MRT0-inf (h) 170 ± 29.7 (17.5%) 180 ± 29.4 (16.4%) 255 ± 17.4 (6.82%) AUC0-inf/AUC0-last (%) 113 ± 11.8 (10.4%) 103 ± 0.940 (0.916%) 103 ± 0.940 (0.916%) C0, initial drug concentration; T1/2, half-life; Vss, apparent volume of distribution in the steady-state; Cl, clearance; Tlast, the last time; AUC, area under the curve; MRT, mean residence time.

Species：Human

Isotype：Human IgG4 lambda

Hot selling product：L-Cycloserine  | Exemestane  | Osthole  | Cephalosporin C zinc salt  | Acriflavine  | Aurantio-obtusin  | Glycol chitosan  | Azumolene  | Tylosin  | Dihydroergocristine (mesylate)

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References：

[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]