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
Human IgG4 lambda
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG4 lambda
ELISA, FACS, Functional assay
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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)