Zimberelimab
Based on 1 Customer Validation
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.
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- Pureté: 99.90%
- CAS No.: 2259860-24-5
- Masse moléculaire:144.41 kDa
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
Isotype
Human IgG4 lambda
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
PDCD1/PD-1/CD279
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.
In Vivo
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.
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Animal Model:The human PD-1 knock-in mouse model of MC38 tumors[2]
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Dosage:10 and 20 mg/kg
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Administration:Intravenous injection, BIW*3
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Result:Showed statistically significant anti-tumor effects comparable with Pembrolizumab (HY-P9902).
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Animal Model:Nine male and nine female cynomolgus monkeys[2]
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Dosage:2, 6, and 18 mg/kg
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Administration:Intravenous injection (Pharmacokinetic Analysis)
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Result:Displays long-term effects in cynomolgus monkeys, without differences between males and females.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG4 lambda
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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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).
Chemical Information
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CAS No. 2259860-24-5
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Appearance Liquid
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Masse moléculaire 144.41 kDa
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Color Colorless to light yellow
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SMILES
[Zimberelimab]
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Synonyms
GLS-010; AB-122; WBP-3055
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Livraison
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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Fiche technique (263 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)