2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. Zimberelimab

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

Cat. No.: HY-P99109 Purity: 99.90%
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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.

For research use only. We do not sell to patients.

Zimberelimab Chemical Structure

Zimberelimab Chemical Structure

CAS No. : 2259860-24-5

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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[1][2].

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].

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

Zimberelimab Related Antibodies
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.

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

Animal Model: The human PD-1 knock-in mouse model of MC38 tumors[2]
Dosage: 10 and 20 mg/kg
Administration: Intravenous injection, BIW*3
Result: Showed statistically significant anti-tumor effects comparable with Pembrolizumab (HY-P9902).
Animal Model: Nine male and nine female cynomolgus monkeys[2]
Dosage: 2, 6, and 18 mg/kg
Administration: Intravenous injection (Pharmacokinetic Analysis)
Result: Displays long-term effects in cynomolgus monkeys, without differences between males and females.
Clinical Trial
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Zimberelimab]
Shipping

Shipping with dry ice.
Storage

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

Purity: 99.90%

COA (231 KB)

Handling Instructions (2659 KB)
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Zimberelimab Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zimberelimab2259860-24-5GLS-010 AB-122 WBP-3055GLS010GLS 010AB122AB 122AB-122WBP3055WBP 3055WBP-3055PD-1/PD-L1PD-1/Programmed death-ligand 1non-small cell lung cancerNSCLCHodgkin lymphomasolid tumorsInhibitorinhibitorinhibit

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