Cetrelimab
Based on 1 Customer Validation
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo.
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- Pureté: ≥99.0%
- CAS No.: 2050478-92-5
- Masse moléculaire:144.76 kDa
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Human IgG4 kappa
Human
PDCD1/PD-1/CD279
Cetrelimab (0.01-30 nM; 5 d) binds to endogenous PD-1 on activated CD4+ and CD8+ T cells with EC50s of 0.16-0.22 µg/mL and 0.17-0.22 µg/mL, respectively[1].
Cetrelimab (0.01-30 μg/mL; 24 h) reverse PD-1-mediated suppression of TCR signaling in Jurkat-PD-1 NFAT reporter cells with CHO-K1 expressing PD-L1[1].
Cetrelimab (0.001-100 nM; 6 d) increases IFN-γ, IL-2, and TNF-α with EC50s of 0.08 ng/mL, 0.07 ng/mL, and 0.02 ng/mL, respectively[1].
Cetrelimab binds to PD-1 in cynomolgus with a Kd value of 0.9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cetrelimab (10 mg/kg; i.p.; once every 5 days for 30 d) results significant increases in peripheral blood CD8+ T cells in patient-derived xenograft (PDX) lung model in mice[1].
Cetrelimab (10-100 mg/kg; i.v.; once weekly for 5 weeks) has well tolerance in cynomolgus model[1].
Cetrelimab (0.1-10 mg/kg; i.v.; single dose, monitored for 57 d) shows an nonlinear pharmacokinetics (PK) in cynomolgus, possibly attributable to target-mediated drug deposition (TMDD)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hPD-1KI model with mouse PD-1 ECD replaced by the human PD-1 ECD[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; single dose at day 7 after tumor implantation
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Result:hPD-1KI mice develop normally and have no immune abnormalities.
Significantly lowered tumor volume at Day 21.
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Animal Model:Patient-derived xenograft (PDX) LG1306 lung model in mice[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; every 5 days for 6 cycles
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Result:Significantly reduced patient-derived tumor volume by 32%.
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Animal Model:Good Laboratory Practice (GLP) toxicity study in cynomolgus[1]
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Dosage:0, 10, 30, or 100 mg/kg
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Administration:Intravenous injection; once weekly for 5 weeks
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Result:Showed well tolerance in cynomolgus.
| 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 kappa
ELISA, FACS, Functional assay
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Immobilized Human PD-1 Protein (ECD, His Tag) can bind Cetrelimab. The EC50 for this effect is 5.75 ng/mL. -
Flow cytometric analysis of 1X106 10 ng/mL PMA and 1 μg/mL Ionomycin co-stimulated Jurkat cells(24h) labeling Cetrelimab (HY-P99499, 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 kappa (HY-P99003, 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. 2050478-92-5
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Appearance Liquid
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Masse moléculaire 144.76 kDa
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Color Colorless to light yellow
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SMILES
[Cetrelimab]
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Synonyms
JNJ 63723283; JNJ 3283
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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 (262 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)
Cetrelimab Related Classifications
HY-P99499 Related Classifications
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